bluuebunny/crossref_metadata_2025 huggingface dataset:
The Anti‐inflammatory Activity of N‐Substituted Indazolones in Mice
Authors: Tse Elaine , Butner Lori , Huang Yunsheng , Hall Iris H.
Published: October 2006

N‐Substituted indazolones were shown to be potent anti‐inflammatory and analgesic agents in mice at 8 mg/kg. In addition, the agents were able to protect against death caused by endotoxins similar to those found in chronic infections. In part, the ability of these agents to suppress the inflammatory process is due to their blockage of cytokine release, e.g. TNFα and IL‐1, as well as their inhibition of high affinity binding to receptors on target cells of inflammation. Suppressing these receptors can be linked to the inhibition by the agents of lysosomal hydrolytic enzymes, prostaglandin cyclooxygenase and 5°‐lipoxygenase activities. Free radical generation involved in inflammation was also stabilized in the presence of most of these agents.
New Antifolate 4,4′‐Diaminodiphenyl Sulfone Substituted 2,4‐Diamino‐5‐benzylpyrimidines. Proof of Their Dual Mode of Action and Autosynergism
Authors: Wiese Michael , Schmalz Dietmar , Seydel Joachim K.
Published: October 2006

New 4,4′‐diaminodiphenylsulfone substituted 2,4‐diamino‐5‐benzylpyrimidines were synthesized. These compounds are highly active inhibitors of both bacterial dihydrofolate reductase (DHFR) and dihydropteroic acid synthase (SYN). The simultaneous inhibition of both enzymes leads to autosynergism in whole cells in the same way as known for combinations of sulfonamides with trimethoprim. The inhibitory activity is demonstrated in cell‐free systems of DHFR and SYN derived from various species (M. lufu, E. coli, C. albicans) and in whole cell systems of the mycobacterial strain M. lufu. The compounds are rare examples for the combination of two mechanisms of action in one molecule.
Synthesis and Anti‐inflammatory Evaluation of New Sulfamoylheterocarboxylic Derivatives
Authors: Díaz Juan A. , Morante M. Esther , Vega Salvador , Darias Victoriano , Abdala Susana , Delgado Laura , de las Heras Beatriz , Villar Angel , Vivas José María
Published: October 2006

A series of new sulfamoylthiophene and sulfamoylpyrazole carboxylic acid derivatives was synthesized. Some of these compounds show interesting analgesic properties and significant nonsteroidal anti‐inflammatory activities in several models of inflammation.
Aziridine‐2,3‐dicarboxylic Acid Derivatives as Inhibitors of Papain
Authors: Schirmeister Tanja
Published: October 2006

Aziridine‐2,3‐dicarboxylates and N‐acylated derivatives have been evaluated as potential irreversible inhibitors of the cysteine proteinase papain. Dependence of inhibition activity on stereo‐chemistry of the aziridine moiety has been analyzed. Whereas unsubstituted (R,R)‐ and (S,S)‐ diethyl aziridine‐2,3‐dicarboxylates (5) and (2) show no significant difference in inactivation the derivative acylated with BOC‐(S)‐Phe (BOC‐(S)‐Phe‐(S,S)‐Azi) (10) shows a 6 fold higher activity than the diastereomer BOC‐(S)‐Phe‐(R,R)‐Azi (11). Analogs acylated with Z‐ or BOC‐(S)‐Ala (9, 8) have lower second‐order rate constants, indicating binding of the amino acid moiety of the inhibitors to the S2 subsite of the enzyme.
2‐Anthracenonyl Acetic Acids as 5‐Lipoxygenase Inhibitors
Authors: Prinz Helge , Müller Klaus
Published: October 2006

The synthesis of 2‐substituted anthracenonyl acetic acid (2‐AA) derivatives is described. The key step is the Marschalk reaction of 1‐hydroxy‐8‐methoxy‐anthracenedione with glycolic acid. After protection of the resulting 2‐anthracenonyl acetic acid derivative, the 2‐monoalkylated derivatives are selectively obtained by direct alkylation. The methodology proves quite general and allows for the introduction of various substituents onto the 2‐position of the carboxylic side chain. Reduction of the anthracenediones proceeds with concomitant protecting group removal and provides final 2‐AA products in good yields. The results of initial biological studies demonstrate enhanced 5‐lipoxygenase inhibition compared to anthralin.
Investigations on the Pathway of the Fluorescence Reaction of a Pharmaceutically Important 1,3‐Diamine with 2‐Benzoylbenzaldehyde
Authors: Troschütz Reinhard , Heinemann Oliver
Published: October 2006

The reaction of 2‐benzoylbenzaldehyde (1) with primary diamine 2, generated by rearrangement and hydrolysis of Oxazepam, in CD3OD leads to intensely fluorescing deuterated isoindoloquinazolines 3 and 4. Reduction of ethyl 2‐benzoylbenzoate (5) with LiAlD4 followed by oxidation with MnO2 yields 2‐benzoylbenz[D]aldehyde (7). The condensation of 7 with diamine 2 leads to isoindoloquinazoline 12, free of deuterium. On the basis of these experiments a plausible pathway is proposed for the “fluorescence reaction”.
Phosphono Analogues of Glutathione as New Inhibitors of Glutathione S‐Transferases
Authors: Kunze Thomas
Published: October 2006

Phosphono‐analogues of glutathione containing the O=P(OR)2 moiety in place of the cysteinyl residue CH2SH 1a–1d were prepared by solution phase peptide synthesis. Benzyl, benzyloxycarbonyl, and tert‐butyl protecting groups were used to mask the individual amino acid functional groups. The formation of peptide bonds was achieved by the usual peptide synthesis via activation of carboxylic functions with cyclohexylcarbodiimide and subsequent reaction with free amino groups. The thus obtained, fully‐protected peptides were each purified by normal phase column chromatography. Deprotection was accomplished by hydrogenolysis and by treatment with HBr/acetic acid yielding the desired phosphonic acid diester 1a–1d. The inhibition of the glutathione conjugation of 1‐chloro‐2,4‐dinitrobenzene by human placental glutathione S‐transferase was studied by determining the IC50 values of the new glutathione analogues. The IC50 values were 291 μM, 139 μM, 64 μM, and 21 μM for the dimethyl, diethyl, diisopropyl, and di‐n‐butyl esters, respectively. The results clearly show that the formal substitution of the glutathione thiol function by phosphonic acid esters leads to a new class of glutathione S‐transferase inhibitors. Further investigations directed at the question of whether or not these glutathione analogues are suitable for a modulation in chemotherapy are in progress.
Syntheses, Calcium Channel Antagonist and Anticonvulsant Activities of Substituted 1,4‐Dihydro‐3,5‐pyridinedicarboxylates Containing Various 3‐Alkyl Ester Substituents
Authors: Yiu Sai‐Hay , Knaus Edward E.
Published: October 2006

A group of 3‐alkyl 5‐isopropyl 4‐aryl‐1,4‐dihydro‐2,6‐dimethyl‐3,5‐pyridinedicarboxylates 10–20 containing an amine, quaternary ammonium, aryl(heteroaryl)alkenyl, 4 ‐ (4‐fluorophenyl)‐piperazin‐1‐yl or methoxy moiety in the C‐3 alkyl ester R‐substituent in combination with a C‐4 phenyl ring bearing a 2,3‐Cl2, 3‐NO2, 3‐NMe2, 4‐NMe2 or 3,4,5‐(OMe)3 X‐substituent were prepared using the Hantzsch 1,4‐dihydropyridine reaction. In vitro calcium channel antagonist activity (CCA) was determined using a guinea pig ileum longitudinal smooth muscle assay. In the C‐4 3‐nitrophenyl series of compounds, the C‐3 ester R‐substituent was a determinant of CCA activity where the relative potency order was −CH2CH2CH=C‐(2‐methylphenyl)2 ± −CH2CH2NMe2.HCl > −CH2CH2CH=C‐(3‐methyl‐2‐thienyl)2 > −CH2CH2+NMe3 I−. The position and nature of the C‐4 phenyl X‐substituent, were also determinants of CCA activity where the relative activity order was 3‐NMe2 > 4‐NMe2 > 3,4,5‐(OMe)3. Anticonvulsant activities were determined in mice using the subcutaneous metrazol (scMet) and maximal electroshock (MES) screens. The compounds investigated were generally not effective for protecting againist scMet induced seizures, except for 10 {X = 2,3‐Cl2, R = 2‐[4‐(4‐fluorophenyl)piperazin‐1‐yl]ethyl} and 14a (X = 3‐NMe2.HCl, R = CH2CH2OMe), which exhibited modest activity. Compound 11a (X = 3‐NO2, R = −CH2CH2NMe2.HCl) was the most effective agent in the MES screen. All of the compounds investigated, except for 11b (X = 3‐NO2, R = −CH2CH2+NMe3 I−, Kp = 0.15), are lipophilic with n‐octanol/aqueous phosphate buffer (pH = 7.4) partition coefficients (Kp) in the 121–424 range relative to the reference drug nimodipine (Kp = 187). The structure‐activity relationships acquired reinforce the concept that calcium is only one of several factors that are involved in seizure generation.
Synthesis and Smooth Muscle Calcium Channel Effects of Dialkyl 1,4‐Dihydro‐2,6‐dimethyl‐4‐aryl‐3,5‐pyridinedicarboxylates Containing a Nitrone Moiety in the 4‐Aryl Substituent
Authors: Anana Raymond D. , Ng Helen , Howlett Susan E. , Knaus Edward E.
Published: October 2006

A group of dialkyl 1,4‐dihydro‐2,6‐dimethyl‐4‐{3‐ (or 4‐)[[(Z)‐N‐oxo‐N‐[4‐substituted‐phenylmethylene (or vinylmethylene)]‐λ5‐azanyl]phenyl}‐3,5‐pyridinedicarboxylates] 7a–n were synthesized. Reaction of the C‐4 nitrophenyl compounds 6a–d with an aryl Grignard reagent afforded the corresponding nitrone derivatives 7a–e. Alternatively, reaction of the aryl hydroxylamine compounds 8a–b prepared by reduction of the nitrophenyl compounds 6c–d with Zn/NH4Cl, or the aryl hydroxylamine compounds 8c–d prepared by reduction of the nitrophenyl compounds 6e–f with 5% rhodium‐on‐charcoal and 65% hydrazine hydrate, with a 4‐substituted‐benzaldehyde, benzaldehyde or acrolein afforded the respective nitrone compounds 7f–n. In vitro calcium channel (CC) antagonist activities were determined using the guinea pig ileum longitudinal smooth muscle assay. This class of compounds containing a nitrone moiety on the 1,4‐dihydropyridine C‐4 phenyl ring exhibited CC antagonist activities (10−5 to 10−9 M range) relative to the reference drug nifedipine (IC50 = 1.43 × 10−8 M). Structure‐activity relationships showed that the position of the nitrone moiety on the C‐4 phenyl ring was a determinant of CC antagonist activity where the potency order was always meta‐nitrone > para‐nitrone. The effect of the ester alkyl substituent was variable depending upon whether the nitrone substituent was at the meta or para‐position (meta‐nitrone, Et > i‐Pr ≈ Me; para‐nitrone, i‐Pr > Me ≈ Et). In the diethyl ester series of compounds having a meta‐nitrone moiety, the difference in potency for the various R2‐nitrone substituents varied by a factor of 15‐fold (IC50 = 1.51 × 10−7 to 9.84 × 10−9 M range) (4‐Cl‐C6H4‐±4‐Me‐C6H4‐ ≈ C6H5‐≥4‐O2N‐C6H4‐ 4‐F3C‐C6H4‐>CH2=CH‐). Whole‐cell voltage‐clamp studies using isolated guinea pig ventricular myocytes indicated that, the 4‐{3‐[(Z)‐N‐oxo‐N‐(phenylmethylene)‐λ5‐azanyl]‐phenyl} compound 7c (10 μM) is a calcium channel antagonist which decreased the calcium current (Ica).
Synthesis and in vitro anti‐HIV Activity of Certain 2‐(1H‐Benzimidazol‐2‐ylamino)pyrimidin‐4(3H)‐ones and Related Derivatives
Authors: Badawey El‐Sayed A. M. , Kappe Thomas
Published: October 2006

In an ongoing effort to develop novel non‐nucleoside human immunodeficiency virus inhibitors, a series of substituted 2‐(1H‐benzimidazol‐2‐ylamino)pyrimidin‐4(3H)‐ones and related derivatives were synthesized via cyclocondensation of 2‐guanidino‐1H‐benzimidazole with diethyl ethoxymethylenemalonate, substituted diethyl malonates, some β‐keto esters and 2‐acetylbutyrolactone. From these series of compounds, 2‐(1H‐benzimidazol‐2‐ylamino)‐6‐hydroxy‐5‐phenylpyrimidin‐4(3H)‐ones (5f, NSC 666286) was confirmed to have a moderate in vitro anti‐HIV activity.
Non‐steroidal Anti‐inflammatory Agents, Part 24[1] Pyrrolidino Enaminones as Models to Mimic Arachidonic Acid
Authors: Dannhardt Gerd , Bauer Adrea , Nowe Ulrike
Published: October 2006

The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5‐lipoxygenase. According to the structure‐activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern of the heterocyclic moiety and of the phenyl group. Compound 4c is the most efficient inhibitor of cyclooxygenase. For the binding profile the unfolded conformation of arachidonic acid and the energy‐minimized conformations of flurbiprofen, diclofenac, ML 3000, and lead compound 4a were compared. In addition to known structural features, similar distances of the carboxylic acid function and the phenyl residue were found as hypothesized to explain the interaction with the active sites of the enzyme. The inhibition of cyclooxygenase was determined in a bovine thrombocyte intact cell assay and that of 5‐lipoxygenase using intact bovine PMNLs.
SAR Studies on the Potent and Selective Muscarinic Antagonist 2‐Ethylthio‐2,2‐diphenylacetic Acid N,N‐Diethylaminoethyl Ester
Authors: Scapecchi Serena , Angeli Piero , Dei Silvia , Ghelardini Carla , Gualtieri Fulvio , Marucci Gabriella , Paparelli Fiorella , Romanelli M. Novella , Teodori Elisabetta
Published: October 2006

Molecular modification of the potent and selective muscarinic antagonist 2‐ethylthio‐2,2‐diphenylacetic acid N,N‐diethylamino‐ethyl ester was performed in order to identify M2 selective antagonists able to cross the blood brain barrier and potentially useful in the treatment of Alzheimer's disease. Modifications included substitution or hydrogenation of one of the phenyl rings as well as their incorporation in a tricyclic system. In general the changes introduced were detrimental for both affinity and selectivity. Only a modest M2 selectivity is present in some compounds that, on the other hand, carry a quaternary ammonium group which precludes their penetration into the brain.
The Oriented Development of Antituberculotics: Salicylanilides
Authors: Waisser Karel , Matyk Josef , Divišová Hana , Husáková Petra , Kuneš Jirí , Klimešová Vera , Kaustová Jarmila , Möllmann Ute , Dahse Hans‐Martin , Miko Milan
Published: October 2006

On the basis of our previous results 22 salicylanilides were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The Free‐Wilson method was used to evaluate structure‐antimycobacterial activity relationships. 4‐Chloro‐N‐(4‐propylphenyl)salicylamide and 5‐chloro‐N‐(4‐propylphenyl)salicylamide were selected for preclinical studies.
Brüche an Isolierglasscheiben – ein thermisches Problem
Authors: Béguin Gilbert H.
Published: October 2006

Beim Fassadenbau liegt der Trend eindeutig auf vermehrtem Gebrauch von Glas. Dies schafft neuartige Probleme. Der Beitrag stellt einige Schadensfälle in Form von Glasbrüchen während der kalten Jahreszeit vor. In jedem Falle traten die Brüche am inneren Float‐Glas auf. Als Ursachen wurden zunächst mechanische Einflüsse vermutet. Messungen zeigten die Wirkung dieser Faktoren als geringfügig. Deshalb wurden dann thermische Einwirkungen vermutet. Zur Untersuchung wurden zwei an den Rändern verbundene Scheiben als zwei thermisch gekoppelte halbunendliche Glasscheiben modelliert. Die entsprechenden Fourier‐Gleichungen wurden mit der Laplace‐Transformation behandelt. Die Berechnungsresultate zeigen bei starkem Wärmeverlust an der äußeren Scheibe das Auftreten von Zugspannungen am Rande der inneren Floatscheibe. Zwei Annahmen für den Verlauf des Wärmeverlustes wurden betrachtet. Die Ergebnisse sind in Graphiken dargestellt.
Autobiographien von Apothekern als Quelle für die Wissenschaftsgeschichte
Authors: Friedrich Christoph
Published: October 2006

The aim of this paper is to demonstrate the importance of autobiographies of dispensing chemists for the history of science. The analysis of the autobiographies of E. W. Martius, D. H. Hoppe, F. T. Kützing and other pharmacists of the 18th and 19th centuries shows, that these books give many informations about the history of medicine, chemistry or botany. The memoirs of pharmacists, published in the later 19th and 20th centuries, for example by Th. Fontane or by H. Sudermann, are especially interisting origins for the history of pharmacy.
Jesuiten zwischen Religion und Wissenschaft
Authors: Blum Paul Richard
Published: October 2006

Natural sciences and natural philosophy of the Jesuits are based on theology. At least the concept of God is an integral part of their theoretical structure. Examples are taken from Rudjer Boskovic, Honoré Fabri and Nicolaus Cabeus. In fact, the Jesuits, e.g. Theophil Raynaud, dealt with natural theology as the spiritual foundation of knowledge independent of revelation. But natural theology, as in Raimundus Sabundus, has an anthropocentric and hence moral dimension: it links knowledge with religion. ‘Ignatius of Loyola influenced decisively the Jesuits’ concept of science and its relationship to religion through his Spiritual Exercises in which meditation and religious practice are developed into a technique and a scientific approach to faith.
On the Structure of a Scientific Golden Age Social Change, University Investments and Germany's Discontinuous Rise to 19th Century Scientific Hegemony
Authors: Willink Bastiaan
Published: October 2006

In diesem Beitrag werden Indikatoren vorgeschlagen für die schwankende Zuwachsrate des Wachstums der Wissenschaften in Deutschland im 19. Jahrhundert. Einer Analyse der Entwicklung des deutschen Universitätswesens, die insbesondere die Zu‐ und Abnahme der Zahl der Universitätslehrer und der finanziellen Aufwendungen berücksichtigte, sind erklärende Faktoren entnommen worden. Der Aufstieg des Wirtschaftsbürgertums sowie die Zusammenarbeit Bismarcks mit den National‐Liberalen um 1870 bildeten die Grundlage für das Wachstum nach 1860. Wenn möglich, werden Vergleiche mit den zwei damals wichtigsten rivalisierenden Staaten, Großbritannien und Frankreich, angestellt.
Prestige und gemeiner Nutzen Universitätsgründungen im deutschen Spätmittelalter
Authors: Schwinges Rainer Christoph
Published: October 2006

The medieval German university entered the picture late but thereby as a new and third type of university in Europe besides Paris and Bologna: This was the ruler‐controlled ‘Four‐Faculties‐University’, which powerfully integrated the socially very different associations of liberal arts, theology, medicine, and law. From the beginning on the ‘German type’ was tied to the princely founder, his court, his dynasty, and his territory (in some cases also to the municipal leadership), and it was politically subjected to his will. All foundations produced prestige and dynastic need at first rather than public need (utilitas publica), respectively the advancing of common learned education and science. The great royal dynasties of Luxembourg, Habsburg, and Wittelsbach began founding in Prague, Vienna, and Heidelberg. Up to 1506 all the seven prince electors, some more important princes and big towns of the Holy Roman Empire had their university or had relations to a university. Public need was rather an indirect result: university students utilized surprisingly strongly the possibilities offered by the subsequent university foundations in Germany ‐ about 200.000 people during a long‐term 15th century. However, it has to be thought over in the history of science and effectivity of the German universities in a European frame, that more than 80% of them were ‘only’ students of arts.
Platon im Arzneibuch und der Heller am Tresen Pharmazie im 16. Jahrhundert zwischen Humanismus, Stadtgesellschaft und Ökonomie
Authors: Müller‐Jahncke Wolf‐Dieter
Published: October 2006

The study focuses on the development of pharmacopoeas during the early modern time. First, the >Nouvo Receptario< of 1499 came out in Florence as the first printed pharmacopoea of a north‐Italian town, edited by the guild of medicins and apothercaries. Following trading routes the idea of >pharmacopoea< arrived in Nuremberg, where the counsil of the town asked the humanist Valerius Cordus to prepare such a book. Printed in 1546, it quickly became the standard in preparing medicines for other towns in southern Germany. At Augsburg, a wealthy and powerful town, the physicians wrote their own pharmacopoea which was printed in 1564. The comparison of the three pharmacopoeas shows that its printing depended on the social stucture and the financial aspects of each town. But even if the apothecaries, the doctors or the mayors were trained in the humanistic tradtion, the materia medica still continued in the arabic tradition, i.e. the old drugs and preparations remained in these pharmacopoeas, probably for financial reasons.
Alexander von Humboldt, die Natur als ‚Kosmos’︁ und die Suche nach Einheit. Zur Geschichte von Wissen und seiner Wirkung als Raumgeschichte
Authors: Daum Andreas
Published: October 2006

Recent historiography has demonstrated a growing sensitivity toward space as a geographical and cultural category. The following article expands on this theme by focusing on Alexander von Humboldt and his understanding of nature as >cosmos<. Humboldt's cosmic concept stressed the interrelatedness of all natural phenomena and their historicity. Humboldt regarded both as dependent on specific spatial conditions. In his view, the same held true for the ideas about nature, the Weltanschauungen, that evolved in history. Against this background, >Humboldtian science< should not be reduced to a mere empiricist approach of interpreting systematically collected data. >Humboldtian science< was fundamentally a concept that paid attention to the formulation of knowledge as well as to the effects and the esthetic impact of that knowledge in geographical and cultural spaces.

Along these lines, this articles argues for adopting a Humboldtian view in observing the spatial dimensions of history. Three ramifications of Humboldtian ideas into the culture of the nineteenth century serve as examples of how we might ourselves employ such a view: The transfer of Humboldtian ideas into the field sciences of Australia; the appeal of Humboldtian in the botanical and meteorological exploration of the American West and its German‐American community; and, finally, the reading of Humboldt in Germany's popular culture during the last third of the nineteenth century that generated a »cosmic understanding« of evolution different from Darwin's theory. In all cases, geographical and cultural spaces strengthened the receptiveness for >Humboldtian science< not only to satisfy the need for knowledge; beyond that, Humboldt's ideas nourished an esthetic perception of nature, and they served as a vehicle for the ideological search for unity in nature and human society.
Kabinett – Seminar – Institut: Raum und Rahmen des forschenden Lernens
Authors: Schubring Gert
Published: October 2006

The paper examines the transition from the traditional forms of learning at German universitites to the specialized research‐oriented forms estahlished during the 19th century. The first transition occurred by complementing the passive form of listening in the Hörsaal with the active studies in the Seminars. While the Seminars remained largely restricted to the humanities and to mathematics, another transition took place in the exact sciences: here, cabinets ‐ originally service facilities for demonstrations by professors during their lectures ‐ were first changed to become Praktika providing students with space for experiments of their own, and were later transformed into Institutes combining all research and study facilities necessary for the by now differentiated and specialized disciplines. The impressive palace‐like buildings for chemistry and physics institutes became an incentive for other, less experimental disciplines to obtain suitably representative buildings as well.
Eine naturwissenschaftliche Forschungsbibliothek des 18. Jahrhunderts: Die Bibliothek der ‚Naturforschenden Gesellschaft’︁ zu Jena
Authors: Ziche Paul , Büch Gabriele , Kenklies Karsten , Neuper Horst , Breidbach Olaf
Published: October 2006

The ‚Naturforschende Gesellschaft’︁, founded in 1793, proved instrumental for the development of science at the University of Jena around 1800. Its library can be considered as one of its most important facilities provided for research and for the education of students. Since this library has been preserved almost without losses, we can ask whether this library served the purpose of a research library in the newly established field of ‚science’︁. In consequence, the role of scientific societies and the genesis of specialised libraries in the area of science can be investigated in an exemplary case, with implications for the concept of scientific research around 1800.
Der Freundschaftsvertrag zwischen dem Museum für Naturkunde Berlin und dem Naturhistorischen Museum Budapest und die Entwicklung einer naturhistorischen Museologie
Authors: Jahn Ilse
Published: October 2006

Scientific cooperations between the museums of natural history in Berlin and in Budapest are described. Already in 19th century, for instance, the specialists of zoological Taxonomy Edmund Reitter (coleopterologist), Geza von Horváth (helminthologist) and Ludwig von Mehély (herpetologist) intensively communicated with the Berlin Zoologists Julius Weise, Karl August Möbius and Anton Collin. After World War II the mueums have been continued using the special collections to their mutual benefit, and when in 1956 the Hungarian collections were disturbed by Soviet military actions, Hungarian zoologists asked for assistance with exchanging specialists and well destined items of their collections. This way in 1963 there have been officially arranged both yearly visits to the museums in Berlin and Budapest and cooperations not only on taxonomy but also on general museological research like problems of modern exhibitions and their evaluating. In 1973, the Berlin museum also participated in the Dictionarium museologicum (1986) initiated by the Hungarian museologist István Eri.
Über deutsch‐ungarische Beziehungen der Medizin im Zeitalter der Aufklärung ‐ zugleich ein Beitrag zur Geschichte der Pestinokulation
Authors: Schultheisz Emil
Published: October 2006

The influence of German science and medicine on the development of Hungarian medicine in the age of Enlightenment has been extraordinary strong. Many Hungarian medical students staid in German medical faculties. The medical interrelationships between Germany and Hungary in the 18th century are discussed in an overview according to following dimensions: education of protestant Hungarian medical students at German »Aufklaerungs‐Universitaeten«, practical and theoretical resonance, membership of scientific societies, personal contacts and correspondence. Outstanding personalities of this aera were Daniel Fischer, István Weszprémi, Abraham Vater. Special attention is given to a new idea: inoculation against plague as first described by A. Vater in his work Blattern‐Beltzen (1721). Thirty years later I. Weszprémi published his original conception ‐ independently from Vater ‐ in the Tentamen de inoculanda peste (1755).
Der medizinische Wissensaustausch zwischen Siebenbürgen und anderen europäischen Ländern im Spiegel des Auslandsstudiums und der ärztlichen Ausbildung der Siebenbürger vor der Gründung der Klausenburger Universität (1872)
Authors: Offner Robert
Published: October 2006

The first perpetual university in Transylvania was founded rather late compared to European standards, namely only in 1872 in Klausenburg (Cluj, Kolozsvár). Through the centuries, the social request for physicians was satisfied by the education of Transylvanian students at foreign universities and by the immigration of physicians from abroad. Concerning the period from 1180 to 1849, we know about 7145 Transylvanian students at more than 80 different universities of the Occident. Thereof, 412 physicians and 219 surgeons can be documented by their names. The ranking list of the most frequented medical faculties (Vienna, Padova, Leyden, Utrecht, Jena, Lipsia, Erlangen, Frankfort‐on‐Oder, Goettingen, Basel etc.) proves that all of these medical men received their professional education (being sponsored socially) from the then most excellent foreign universities. Thus, studies abroad guaranteed continual transfer of knowledge from Western to Eastern Europe. This situation seems to partially have compensated the disadvantages of lacking own Transylvanian universities ‐ at least from the quality point of view, so that the professional standard of the education of doctors working in Transylvania used to correspond to the highest level of European medicine.
Intra-anal collagen injection for the treatment of faecal incontinence
Authors: Stojkovic S G , Lim M , Burke D , Finan P J , Sagar P M
Published: October 2006

Background

Intra-anal injectable agents have been used to treat faecal incontinence. The aim of this study was to report the experience of a cohort of patients who underwent intra-anal injection of collagen and to determine which patients benefited from the technique.

Methods

Data, including age, sex, incontinence score, classification of incontinence, baseline resting pressure and vector volume, were collected prospectively for 73 consecutive patients (59 women) undergoing intra-anal collagen injection. Patients were reviewed after treatment and incontinence scores documented. A proportion of patients also underwent repeat anorectal physiological testing 8 weeks after the procedure.

Results

At a median follow-up of 12 months after the intra-anal injection, 63 per cent of patients had an improved incontinence score and 73 per cent reported an overall improvement in symptoms. Logistic regression showed that older age and idiopathic faecal incontinence were predictors of a successful outcome (P = 0·042 and P = 0·048 respectively).

Conclusion

Intra-anal collagen injection appears to have a role in the treatment of faecal incontinence. The majority of patients can expect both objective and subjective improvement. The best results are achieved in older patients and in those with idiopathic incontinence.
Silica Gel Triggered Transformations of 3‐Methylenecyclopropylmethyl Sulfonates to 3‐Methylenecyclobutyl Analogues: Experimental and Computational Studies
Authors: Shao Li‐Xiong , Li Yu‐Xue , Shi Min
Published: October 2006

Methylenecyclopropylcarbinols 1 treated with sulfonyl chloride and Et3N form the sulfonated products 3 in almost quantitative yields, which can be transformed to the corresponding 3‐methylenecyclobutyl sulfonates 4 with silica gel chromatography work‐up. The rational explanation was proposed on the basis of computational studies.
Redox‐Controlled Interaction of Biferrocenyl‐Terminated Dendrimers with β‐Cyclodextrin Molecular Printboards
Authors: Nijhuis Christian A. , Dolatowska Karolina A. , Ravoo Bart Jan , Huskens Jurriaan , Reinhoudt David N.
Published: October 2006

This paper describes the synthesis and electrochemistry of biferrocenyl‐terminated dendrimers and their β‐cyclodextrin (β‐CD) inclusion complexes in aqueous solution and at surfaces. Three generations of poly(propylene imine) (PPI) dendrimers, decorated with 4, 8, and 16 biferrocenyl (BFc) units, respectively, were synthesized. A water‐soluble BFc derivative forms stable inclusion complexes with β‐CD. The intrinsic binding constant is Ki=2.5×104 M−1. The BFc dendrimers were solubilized in water by complexation of the end groups with β‐CD, resulting in large water‐soluble supramolecular assemblies. Cyclic voltammetry (CV) and differential pulse voltammetry (DPV) showed that all the end groups are complexed to β‐CD. Adsorption of the dendrimers at self‐assembled monolayers (SAMs) of heptathioether‐functionalized β‐CD on gold (“molecular printboards”) resulted in stable monolayers of the dendrimers due to the formation of multivalent host–guest interactions between the BFc end groups of the dendrimers and the immobilized β‐CD molecules. The number of interacting end groups is 3, 4, and 4 for dendrimer generations 1, 2, and 3, respectively. The complexation of BFc to β‐CD is sensitive to the oxidation state of the BFc unit. Oxidation of neutral BFc‐Fe2(II,II) to the cationic, mixed‐valence biferrocenium BFc‐Fe2(II,III)+ resulted in dissociation of the host–guest complexes. Scan‐rate‐dependent CV and DPV analyses of the dendrimer–β‐CD assemblies immobilized at the β‐CD host surface and in solution revealed that the dendrimers are oxidized in three steps. First, the surface‐β‐CD‐bound BFc moieties are oxidized to the mixed‐valence state, Fe2(II,III)+, followed by the oxidation of the non‐surface‐interacting BFc groups to the Fe2(II,III)+ state. The third step involves the oxidation of all the BFc moieties to the Fe2(III,III)2+ state.
Reusable Catalysts for the Asymmetric Diels–Alder Reaction
Authors: Chollet Guillaume , Guillerez Marie‐George , Schulz Emmanuelle
Published: October 2006

A new method for recycling chiral bis(oxazoline)–copper complexes is described based on the formation of charge‐transfer complexes, their subsequent precipitation, and reuse after addition of new substrates. The conditions to perform this procedure were optimized in the presence of three bis(oxazoline)‐based ligands. When associated with copper salts, these ligands efficiently catalyzed the Diels–Alder reaction between cyclopentadiene and α,β‐unsaturated acyloxazolidinones. These catalysts were successfully recycled up to ten times while maintaining their high activities and enantioselectivities.
Au3SnCuP10 and Au3SnP7: Preparation and Crystal Structures of Au3Sn Heterocluster Polyphosphides.
Authors: Lange Stefan , Nilges Tom
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Lewis Acid Catalyzed Tri‐ and Difluoromethylation Reactions of Aldehydes.
Authors: Mizuta Satoshi , Shibata Norio , Ogawa Shinichi , Fujimoto Hiroyuki , Nakamura Shuichi , Toru Takeshi
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Nickel‐Catalyzed Bis‐allylation of Internal Alkynes with Triallylindium.
Authors: Hirashita Tsunehisa , Akutagawa Kazuhiko , Kamei Toshiya , Araki Shuki
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
P2O5/SiO2‐Catalyzed One‐Pot Synthesis of Amides from Ketones via Schmidt Reaction under Microwave Irradiation in Dry Media.
Authors: Eshghi Hossein , Hassankhani Asadollah
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Preparation of Diamines of Adamantane and Diamantane from the Diazides.
Authors: Davis Matthew C. , Nissan David A.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Nickel(0)/Imidazolium Carbene Catalyst System for Efficient Cross‐Coupling of Aryl Bromides and Chlorides with Organomanganese Reagents.
Authors: Leleu Anne , Fort Yves , Schneider Raphael
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
New Palladium Complexes with S‐ or Se‐Containing Schiff‐Base Ligands as Efficient Catalysts for the Suzuki—Miyaura Cross‐Coupling Reaction of Aryl Bromides with Phenylboronic Acid under Aerobic Conditions.
Authors: Kostas Ioannis D. , Steele Barry R. , Terzis Aris , Amosova Svetlana V. , Martynov Alexander V. , Makhaeva Natalia A.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A Chiral Iron(II)—Pybox Catalyst Stable in Aqueous Media. Asymmetric Mukaiyama—Aldol Reaction.
Authors: Jankowska Joanna , Paradowska Joanna , Mlynarski Jacek
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Carbonylative Cross‐Coupling Reaction of Ethynylstibane with Aryl Iodides.
Authors: Kakusawa Naoki , Kurita Jyoji
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Asymmetric [3 + 2] Annulations Catalyzed by a Planar‐Chiral Derivative of DMAP.
Authors: Bappert Erhard , Mueller Peter , Fu Gregory C.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A Convenient Synthetic Route to 2‐Aryl‐N‐tosylazetidines (V) and Their ZnX2 (X = I, OTf) Mediated Regioselective Nucleophilic Ring Opening Reactions: Synthesis of γ‐Iodoamines and Tetrahydropyrimidines.
Authors: Ghorai Manas K. , Das Kalpataru , Kumar Amit , Das Animesh
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A New Class of Laser Dyes, 2‐Oxa‐bicyclo[3.3.0]octa‐4,8‐diene‐3,6‐diones, with Unity Fluorescence Yield.
Authors: Wang Chao‐Yu , Yeh Yu‐Shan , Li Elise Y. , Liu Yi‐Hong , Peng Shiuh‐Ming , Liu Shiuh‐Tzung , Chou Pi‐Tai
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Diastereoselective, Vinylogous Mukaiyama Aldol Additions of Silyloxy Furans to Cyclic Ketones: Annulation of Butenolides and γ‐Lactones.
Authors: Kong Ke , Romo Daniel
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Synthesis of Polynuclear Aromatic Compounds Through Net [5 + 5]‐Cycloaddition of 2‐Alkynylarylcarbene Complexes and Enyne—Aldehyde Derivatives.
Authors: Zhang Yanshi , Herndon James W.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Reactivity Series for s‐BuLi/Diamine‐Mediated Lithiation of N‐Boc Pyrrolidine: Applications in Catalysis and Lithiation of N‐Boc Piperidine.
Authors: McGrath Matthew J. , Bilke Julia L. , O'Brien Peter
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
An Approach to the Paal—Knorr Pyrroles Synthesis Catalyzed by Sc(OTf)3 under Solvent‐Free Conditions.
Authors: Chen Jiuxi , Wu Huayue , Zheng Zhiguo , Jin Can , Zhang Xingxian , Su Weike
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
An Efficient Synthesis of Bis(indolyl)methanes (BIAs) Catalyzed by a Recyclable Solid Superacid SO42‐/TiO2 under Solvent‐Free Condition.
Authors: Zeng Xiao‐Fei , Ji Shun‐Jun
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
PdCl2 Immobilized in Ionic Liquids: A Novel and Efficient Catalytic System for Michael Additions of Indoles to α,β‐Unsaturated Ketones.
Authors: Lin Xufeng , Cui Sunliang , Wang Yanguang
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A Facile Synthesis of Linear Benzene‐Fused Bis(tetrathiafulvalene) Compounds and Their Application for Organic Field‐Effect Transistors.
Authors: Gao Xike , Wu Weiping , Liu Yunqi , Qiu Wenfeng , Sun Xiaobo , Yu Gui , Zhu Daoben
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Estrogen Receptor β‐Subtype Selective Tetrahydrofluorenones: Use of a Fused Pyrazole as a Phenol Bioisostere.
Authors: Wilkening R. R. , et al. et al.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A New Photocaging Group for Aromatic N‐Heterocycles.
Authors: Lusic Hrvoje , Deiters Alexander
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Direct Conversion of Esters, Lactones, and Carboxylic Acids to Oxazolines Catalyzed by a Tetranuclear Zinc Cluster.
Authors: Ohshima Takashi , Iwasaki Takanori , Mashima Kazushi
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Synthesis of Substituted Benzoxacycles via a Domino ortho‐Alkylation/Heck Coupling Sequence.
Authors: Martins Andrew , Marquardt Udo , Kasravi Neema , Alberico Dino , Lautens Mark
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Vanadium(III) Chloride as an Effective Catalyst for the Pechmann Reaction.
Authors: Kumar B. Sunil , Kumar P. S. , Srinivasulu N. , Rajitha B. , Reddy Y. Thirupathi , Reddy P. Narsimha , Udupi R. H.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Synthesis of the Thioamide Derivatives of Methyl Vinyl Ketone and Their Cyclization to 2,3‐Dihydro‐4H‐thiopyran‐4‐ones.
Authors: Gros L. , Westerlich S. , Wesolowska A. , Jagodzinski T. S.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
4‐Hydroxyquinolones‐2. Part 91. Synthesis and Properties of Ethyl 1‐Substituted‐ 4‐hydroxy‐6‐methyl‐2‐oxo‐dihydropyridine‐5‐carboxylates.
Authors: Ukrainets I. V. , Sidorenko L. V. , Gorokhova O. V. , Shiskhin O. V.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Enantioselectivity and Diastereoselectivity in Reductive Radical Cyclization Reaction of 3‐(ω‐Iodoalkylidene)‐piperidin‐2‐ones.
Authors: Dressel Martina , Aechtner Tobias , Bach Thorsten
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Ceric Ammonium Nitrate (CAN) Catalyzes the One‐Pot Synthesis of Polyhydroquinoline via the Hantzsch Reaction.
Authors: Ko Shengkai , Yao Ching‐Fa
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Discovery of Protein—Protein Binding Disruptors Using Multi‐Component Condensations Small Molecules.
Authors: Bedjeguelal Karim , Bienayme Hugues , Dumoulin Antoine , Poigny Stephane , Schmitt Philippe , Tam Eric
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Synthesis of Novel 5‐Piperidyl‐substituted 7‐Hydroxy‐3H‐1,2,3‐triazolo[4,5‐d]pyrimidines.
Authors: Kuleshov K. V. , Borovkov K. Yu. , Rodin O. G. , Perevalov V. P.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Novel Reactions to Form an Si—O—Ge Group.
Authors: Ignatovich L. , Muravenko V. , Grinberga S. , Lukevics E.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Structure Elucidation of Two New Diterpenoids from Isodon Phyllostachys: Phyllostacins A (I) and B (II).
Authors: Li Xian , Xiao Wei‐Lie , Huang Sheng‐Xiong , Weng Zhi‐Ying , Shen Yun‐Heng , Han Quan‐Bin , Sun Han‐Dong
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Total Synthesis of Prolycopene, a Novel 7,9,7′,9′‐Tetra‐cis(Z) Carotenoid and Main Pigment of the Tangerine Tomato Lycopersicon esculentum.
Authors: Pattenden Gerald , Robson David C.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
New Stephaoxocane Alkaloids from Stephania longa
Authors: Zhang Hua , Yue Jian‐Min
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
A Flow Process for the Multi‐Step Synthesis of the Alkaloid Natural Product Oxomaritidine: A New Paradigm for Molecular Assembly.
Authors: Baxendale Ian R. , Deeley Jon , Griffiths‐Jones Charlotte M. , Ley Steven V. , Saaby Steen , Tranmer Geoffrey K.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Total and Formal Enantioselective Synthesis of Lyngbic Acid and Hermitamides A and B
Authors: Virolleaud Marie‐Alice , Menant Christine , Fenet Bernard , Piva Olivier
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
N‐Acylated Sulfonamide Sodium Salt: A Prodrug of Choice for the Bifunctional 2‐Hydroxymethyl‐4‐(5‐phenyl‐3‐trifluoromethyl‐pyrazol‐1‐yl) Benzenesulfonamide Class of COX‐2 Inhibitors.
Authors: Singh Sunil Kumar , Vobbalareddy Saibaba , Kalleda Srinivasa Rao , Casturi Seshagiri Rao , Mullangi Ramesh , Ramanujam Rajagopalan , Yeleswarapu Koteswar Rao , Iqbal Javed
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Recent Advances in Microwave‐Assisted Combinatorial Synthesis and Library Generation
Authors: Lange Tim , Lindell Stephen
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.