bluuebunny/crossref_metadata_2025_split huggingface dataset:
Asymmetrische reduktive Aminierung von Cycloalkanonen 8. Mitt. Die EPC‐Synthese arylsubstituierter cis‐4aR, 10bR‐ und cis‐4aS, 10bS‐Octahydrophenanthridine
Authors: Nachtsheim Corina M. , Frahm August W. 
Published: October 2006

AbstractEs wird die EPC‐Synthese der Octahydrophenanthridin‐hydrochloride 4 aus den optisch aktiven 2‐Arylcyclohexanaminen 1 a) unter Pictet‐Spengler‐Bedingungen und b) über die entspr. Formamide 2 und die Hexahydrophenanthridine 3 beschrieben.
Synthese und Oxidation von 3‐(2,5‐Dihydroxyphenyl)‐propylamin‐Derivaten
Authors: Kuckländer Uwe , Bastian Udo 
Published: October 2006

AbstractDie Kondensation des Aldehyds 1 mit CH‐aciden Verbindungen führt zu den Styrol‐Abkömmlingen 2a–j. Aus 2a werden die Amine 5a–e dargestellt. Bei Einwirkung von Luftsauerstoff auf 5a,b bilden sich die Tetrahydrochinoline 8a,b. Durch Oxidation von 5d,e können die Chinone 9a,b dargestellt werden. Die N‐Aryl‐amine 13a–f werden aus 1 über 11 und 12 erhalten. Die Hydrochinone 15a–c cyclisieren ebenfalls oxidativ zu den Chinolinen 17a,b,c. Die Oxidation von 15a,b,c (bzw. 16a,b) liefert die ringoffenen Chinone 18a–c bzw. 19a,b. 18a addiert 2‐Aminothiophenol zu 22, dessen Oxidation ergibt 24.
Acetylpanaxydol und Panaxydolchlorhydrin, zwei neue, gegen L1210‐Zellen cytotoxische Polyine aus Koreanischem Ginseng
Authors: Ahn Byung‐Zun , Kim Shin‐Ii , Lee You‐Hui 
Published: October 2006

AbstractZwei neue gegen L1210‐Zellen cytotoxisch wirksame Polyine wurden aus Koreanischer Ginseng‐Wurzel isoliert. Es handelt sich um 3‐Acetyloxy‐9,10‐epoxyheptadec‐1‐en‐4, 6‐diin (Acetylpanaxydol, ED50= 0.52 μg/ml) und 10‐Chlor‐3,9‐dihydroxyheptadec‐1‐en‐4, 6‐diin (Panaxydolchlorhydrin, ED50= 0.50 μg/ml).
Synthesis of New Annellated Flavonoid Derivatives Possessing Spasmolytic Activity ‐ VII
Authors: Ertan Rahmiye , Göker Hakan , Ertan Mevlüt , Pindur Ulf 
Published: October 2006

Abstract7,8‐Dihydroxyflavone reacts with ethyl 2, 3‐dibromopropanoate to form the new, annellated, 1, 4‐benzodioxanes 1 containing a flavone structural unit. The regioisomers 1a and 1b thus obtained were separated and 1a was converted to the amides 2a–2f. The constitutions of 1 and 2 were elucidated by 500 MHz 1H‐NMR spectroscopy. In the spasmolysis test, 2e showed significant antagonistic effects towards the agonists acetylcholine, barium chloride, and histamine.
1,3‐Diphenylpropane‐1,3‐diamines, IV. Synthesis of 1,3‐Bis(hydroxy‐halogenophenyl)propane‐1,3‐diamines and their Pt(II) Complexes. Part B: Preparation of the Pt(II) Complexes
Authors: Kammermeier Thomas , Wiegrebe Wolfgang 
Published: October 2006

AbstractThe preparation of the Pt(II) complexes of the diamines described in Part A with Cl‐, I‐, SO42−, and water as additional ligands is reported.
1,2‐Dihydro‐4‐chinazolinone aus Anthranilamiden und Oxoverbindungen – Untersuchungen zum Reaktionsverlauf der Ringschlußreaktion
Authors: Lessel Jürgen 
Published: October 2006

AbstractDas Erhitzen der Anthranilsäureamide 1a‐c mit Oxoverbindungen ohne Solvens erlaubt die Synthese der 1,2‐Dihydro‐4‐chinazolinone 8–25, unter drastischeren Bedingungen erfolgt bei β‐Dicarbonylverbindungen eine Eliminierung zu den Methylchinazolinonen 26/27; die Reaktionen verlaufen thermodynamisch kontrolliert. Die aus cyclischen β‐Diketonen erhaltenen Enaminone 28/29 erfahren in Eisessig eine Ringtransformation zu den Chinazolinylpentanonen 34/35, die mit störungstheoretischen Methoden erklärt wird.
New NO‐Donors with Antithrombotic and Vasodilating Activities, VI: Thiazole‐2‐nitrosimines
Authors: Rehse Klaus , Lüdtke Eberhard 
Published: October 2006

Abstract24 new thiazole‐2‐nitrosimines were prepared and described by means of spectroscopical methods (NMR, IR, MS, UV). At pH 7 in cell free systems as well as in platelet rich plasma the compounds are stable against hydrolysis and do not react with the platelet glutathione. The chemical stability is underlined by the mass spectra: M+. is of high intensity and sometimes even forms the base peak (e.g. 8a). Thermal elimination of N2 is of minor importance. The NNO bond in solution is susceptible to cleavage by visible light. The metabolite so formed is able to inhibit the platelet aggregation induced by collagen (Born‐test). Five compounds exhibit this activity in concentrations below 10 μmol/L (IC50). This is due to the release of a NO species, as could be demonstrated by the stimulation of soluble guanylate cyclase in a cell free system (e.g. 8a, KM = 72 μmol/L). In vivo the nitrosimines show antithrombotic properties. Two h after a single oral dose of 8g (60 mg/kg) a 57% inhibition of the laser induced thrombus formation in the mesenteric arterioles of rats is observed. After 8 h a 43% inhibition still is seen.
Building Blocks for the Preparation of Enantiomerically Pure Drugs Containing a Phenylalkylamine Moiety. Synthesebausteine zur Herstellung enantiomerenreiner Arzneistoffe mit Phenylalkylamin‐Partialstruktur
Authors: Bracher Franz , Litz Thomas 
Published: October 2006

AbstractThe enantiomers of chiral drugs may exhibit distinctly different pharmacokinetic and pharmacodynamic properties. Thus, the application of pure enantiomers is desirable in most cases. Therefore, it is necessary to know which enantiomer is the more advantageous one and to work out an economical large scale synthesis of this pure enantiomer. Biocatalytic transformations of prochiral compounds provide an easy and efficient access to chiral, non racemic compounds. Therefore, we fixed upon microbial reductions of carbonyl compounds as the key steps in the preparation of enantiomerically pure building blocks.
Structure‐Activity Relationship Studies of Novel Pyrazolo[1,5‐c][1,3]benzoxazines: Synthesis and Benzodiazepine Receptor Affinity
Authors: Varano Flavia , Catarzi Daniela , Colotta Vittoria , Cecchi Lucia , Filacchioni Guido , Galli Alessandro , Costagli Chiara 
Published: October 2006

AbstractSome 2‐arylpyrazolo[1,5‐c][1,3]benzoxazin‐5‐ones 1 and 5‐oxopyrazolo[1,5‐c][1,3]benzoxazin‐2‐carboxylates 2 were prepared and biologically evaluated for their binding at benzodiazepine receptor (BZR) in rat cortical membranes. Structure‐activity relationship studies suggest that, although proton donor d and proton acceptor a1 are both optional pharmacophoric descriptors, at least one of them must be present for good BZR affinity. When the proton donor d is not present, the heteroatom acceptor a1 is necessary either in the tricyclic core or in the appended substituent at the C‐2 to obtain sub‐micromolar BZR affinity.
New NO‐Donors with Antithrombotic and Vasodilating Activities, Part 16 3‐Amino‐1,2,4‐oxadiazol‐5‐ones as Prodrugs for Hydroxyguanidines
Authors: Rehse Klaus , Bade Stephan 
Published: October 2006

AbstractNineteen 4‐substituted 1,2,4‐oxadiazol‐5‐ones (6a‐s) were prepared as prodrugs for lipophilic hydroxyguanidines which should be metabolized in vivo to nitric oxide. This hypothesis was tested indirectly by measuring the antithrombotic properties of these compounds 2 h after oral administration to rats (60 mg/kg). In mesenteric arterioles seven compounds moderately (≥ 10%) inhibited the formation of thrombi by a laser beam. Maximum effects were observed in 6c (4‐pentyl) and 6f (4‐benzyl). The lack of activity in the corresponding 2‐pentyloxadiazolone 10c, where no formation of nitric oxide seems possible, indirectly suggests that the antithrombotic properties of the title compounds could be mediated by the in vivo formation of nitric oxide.
Dibenz[b,f]azepines, Part 7[1]: Synthesis of New, Potentially CNS Active Dibenz[b,f]azepine Derivatives
Authors: Haász Ferenc , Tóth Zoltán , Galamb Vilmos 
Published: October 2006

AbstractReactions of 5‐carboxamido‐5H‐dibenz[b,f]azepines (1a–1d) with glyoxylic acid methylester methyl hemiacetal (GMHA) led to 5‐(carboxamido‐N‐α‐hydroxy‐acetic acid methyl ester)‐5H‐dibenz[b,f]azepines (2a–2d). The reactions with glycols yielded the oligoethylene glycol derivatives (3,4). The new compounds were screened as anticonvulsants and/or antidepressants (AD).
Search for New Anticonvulsant Compounds, Part 2. Structure‐Activity Relationship Studies of New N‐Substituted Amides of α‐Piperazine‐γ‐Hydroxybutyric Acid as Active Anticonvulsants
Authors: Malawska Barbara , Kulig Katarzyna , Ciechanowicz‐Rutkowska Maria 
Published: October 2006

AbstractIn a search for new anticonvulsants, two series of compounds, viz. derivatives of N‐benzylamides of α‐(4‐phenylpiperazine)‐γ‐hydroxybutyric acid (Aand derivatives of N‐benzylamides of α‐(4‐benzylpiperazine)‐γ‐hydroxybutyric acid (B), were investigated. These amides were obtained by aminolysis of 3‐(4‐phenyl‐, or 4‐benzylpiperazine)‐tetrahydrofuran‐2‐one with primary arylalkylamines (i.e. 2‐phenylethylamine and 2,3,4‐substituted derivatives of benzylamine). Preliminary pharmacological tests, a maximal electroshock (MES) and a subcutaneous metrazole (scMet), and a rotorod toxicity assay were employed. All compounds displayed anticonvulsant activity at range of doses 100–300 mg/kg in the MES screens. In order to point to some structural features correlating with the MES anticonvulsant activity crystal structure analysis followed by conformational analysis was carried out on two representative compounds of series A and B.
Small Peptide Libraries: Combinatorial Split‐Mix Synthesis followed by Combinatorial Amino Acid Analysis of Selected Variants
Authors: Weinberger Heinz , Lichte Ellen , Griesinger Christian , Kutscher Bemhard 
Published: October 2006

AbstractPeptides from small combinatorial libraries, covalently attached to polymeric TentaGel beads, can be directly sequenced using amino acid analysis. For libraries with restricted diversity, generated by the split‐mix synthesis method, the amino acids on a selected single bead identified by pre‐column derivatization with o‐phthaldialdehyde (OPA) correlate directly with the sequence of a given peptide. This is shown on a tripeptide (343 different compounds) and a tetrapeptide (4096 different compounds) library. This method allows for rapid peptide sequence determination without relying on complex encoding strategies.
Bioorganometallic Chemistry – Synthesis and Antitumor Activity of Cobalt Carbonyl Complexes
Authors: Jung Manfred , Kerr David E. , Senter Peter D. 
Published: October 2006

AbstractThe interaction of organometallic compounds with biological systems, generally called bioorganometallic chemistry, is receiving increasing interest. We present the first part of our studies concerning the biological activity of organometallic compounds. Several alkyne‐cobalt carbonyl complexes inhibited the growth of human melanoma and lung carcinoma cell lines. They are more active than uncomplexed dicobalt octacarbonyl, cobalt chloride, or the free ligand. A significant difference in potency towards the lung carcinoma cell line was observed among the cobalt complexes, indicating that the complexed ligand may influence cytotoxic activity. These results suggest that further exploratory work with such cobalt‐alkyne complexes is warranted.
Synthesis and Action on the Central Nervous System of 3‐Substituted 2‐Phenyl‐2,3‐dihydro‐4H‐1,3,2‐benzoxazaphosphorin‐4‐one 2‐Oxide and 2‐Sulfide Derivatives
Authors: Kostka Krzysztof , Porada Marek , Zyner Elzbieta , Pakulska Wanda , Szadowska Anna 
Published: October 2006

AbstractThe synthesis of 3‐substituted 2‐phenyl‐2,3‐dihydro‐4H‐1,3,2‐benzoxazaphosphorin‐4‐one 2‐sulfide derivatives is described. The action of a series 2‐oxide (1–6) and 2‐sulfide (7–12) derivatives on the central nervous system has been evaluated. Compounds 1–4, 6, 7–10 exhibit neuroleptic activity. Derivatives of sulfide series act as antiserotoninergic drugs.
Noncompetitive NMDA Antagonists: A Novel Synthesis of 1‐Phenyltetrahydro‐3‐benzazepines
Authors: Wünsch Bernhard , Nerdinger Sven , Bauschke Gerd , Höfner Georg 
Published: October 2006

AbstractThe key step in the synthesis of the pharmacologically interesting 1‐phenyltetrahydro‐3‐benzazepine skeleton is the Michael addition of (2‐lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n‐butyllithium, to β‐nitrostyrene (6). The reductive ring closure of the nitro acetals 7a,b succeeded with zinc dust and hydrochloric acid to give the 3‐benzazepines 11a,b in good yields. The unsubstituted 3‐benzazepine 11a showed a considerable affinity for the phencyclidine binding site of the NMDA receptor (Ki = 6.41 μM), whereas donor substituents in the aryl moiety (11b,c) reduce the affinity for the NMDA receptor.
Synthesis and Antitumour Activity of New Derivatives of Flavone‐8‐acetic Acid (FAA). Part 2: Ring‐Substituted Derivatives
Authors: Aitken R. Alan , Bibby Michael C. , Double John A. , Laws Andrea L. , Ritchie Robert B. , Wilson David W. J. 
Published: October 2006

AbstractA range of 18 derivatives of flavone‐8‐acetic acid (FAA) with substituents on the 2‐phenyl group have been prepared and their anti‐tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. There was no clear‐cut relationship between in vitro and in vivo activity but the activity in each situation was found to be very sensitive to the precise substitution pattern with closely related isomers giving widely different activities. Some of the compounds, notably 10b,cj, and r, were active in vivo and these require further studies in order to evaluate their potential for development.
Search for New Antiarrhythmic and Hypotensive Compounds. Synthesis, Antiarrhythmic, Antihypertensive, and α‐Adrenoceptor Blocking Activity of Novel 1‐[(2‐Hydroxy‐3‐amino)]‐propylpyrrolidin‐2‐one Derivatives
Authors: Filipek Barbara , Sapa Jacek , Malawska Barbara , Kulig Katarzyna , Antkiewicz‐Michaluk Lucyna 
Published: October 2006

AbstractA series of the derivatives of 1‐[2‐hydroxy‐3‐(4‐phenyl‐1‐piperazinyl)propyl]‐pyrrolidin‐2‐one (MG‐1) was synthesized and tested for electrocardiographic, antiarrhythmic, and antihypertensive activity as well as for α1‐ and α2‐ adrenoceptors binding affinities. Some of the compounds of this series slightly decreased the heart rate, prolonged P‐Q, Q‐T intervals and QRS complex. Only compound 7 (1‐[2‐hydroxy‐3‐(4‐phenyl‐1‐piperazinyl)propyl]‐pyrrolidine) possesses potent antiarrhythmic and a slight hypotensive properties, and affinity for α1‐ and α2‐ adrenoceptor. The results suggest that the antiarrhythmic and hypotensive effect of compound 7 and MG‐1 is related to their adrenolytic properties, and that those properties depend on the presence of a phenylpiperazine moiety.
Novel Carbocyclic Nucleosides Containing a Cyclopentyl Ring. Adenosine and Uridine Analogues
Authors: Balo Carmen , Fernández Franco , Lens Evangelina , López Carmen , Andrei Graciela , Snoeck Robert , Balzarini Jan , De Clercq Erik 
Published: October 2006

Abstractcis‐3‐Aminomethylcyclopentylmethanol (4) was used as a precursor in the synthesis of carbocyclic nucleosides containing adenine, hypoxanthine, 8‐azahypoxanthine, uracil, and 5‐iodouracil bases. None of these compounds had appreciable activity against eighteen viruses in the concentration ranges tested. Two of them showed a weak cytostatic activity against three tumor lines.
Synthesis and Antimicrobial Activity of Some New Anilino Benzimidazoles
Authors: Tunçbilek Meral , Göker Hakan , Ertan Rahmiye , Eryigit Recep , Kendi Engin , Altanlar Nurten 
Published: October 2006

AbstractA series of 2‐(anilino or 2,6‐dichloroanilino)‐1,5(6)‐disubstituted‐1H‐benzimidazoles (1–43) were prepared by reaction of several 2‐chloro‐ or 2‐chloromethyl‐1H‐benzimidazoles with aniline derivatives. The prepared compounds were screened for their in vitro antibacterial and antifungal activities. Compounds 2, 8, and 9 exhibited the best activity.
Tricyclic Heteroaromatic Systems. Pyrazolo[3,4‐c]quinolin‐4‐ones and Pyrazolo[3,4‐c]quinoline‐1,4‐diones: Synthesis and Benzodiazepine Receptor Activity
Authors: Catarzi Daniela , Colotta Vittoria , Varano Flavia , Cecchi Lucia , Filacchioni Guido , Galli Alessandro , Costagli Chiara 
Published: October 2006

AbstractSome pyrazolo[3,4‐c]quinoline‐4‐ones 1–14 and pyrazolo[3,4‐c]‐quinoline‐1,4‐diones 15–17 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The moderate binding activity of 1–5,7,9–10, 13 is attributable to the lack of the optional proton acceptor at position‐1, while the inactivity of the 1,4‐dione derivatives 15–17 is due to the lack of the essential proton acceptor at position‐3. These conclusions confirm the validity of our proposed pharmacophoric model.
New NO‐Donors with Antithrombotic and Vasodilating Activities, Part 17. Arylazoamidoximes and 3‐Arylazo‐1,2,4‐oxadiazol‐5‐ones
Authors: Rehse Klaus , Bade Stephan , Harsdorf Angela , Clement Bernd 
Published: October 2006

AbstractSeven arylazoamidoximes (3), six phenoxycarbonyl derivatives (4), and six 1,2,4‐oxadiazol‐5‐ones (5) have been prepared and their structure and purity established by spectroscopy and elemental analysis. In the EI mass spectra ready elimination of NO from the title amidoximes was observed. A new addition reaction of 3a with hydrochloric acid to 4‐chlorophenylhydroazoamidoxime 7 is described. The compounds were tested for nitric oxide dependent biological properties, i.e. platelet aggregation, antithrombotic effects, and decrease in blood pressure. In arterioles of rats 5/19 compounds inhibited the formation of thrombi with a laser beam by ≥ 20% 2 h after oral administration of 60 mg/kg. Among these are three amidoximes (3a, 3e, 3f), one phenoxycarbonyl derivative (4a), and one oxadiazolone (5a). With the 4‐chlorophenylazoamidoxime 3c a long lasting (24 h) decrease of blood pressure in spontaneously hypertensive rats was observed. Microsomal fractions of rat liver oxidize arylazoamidoximes and generate nitric oxide (e.g. 3a and 3b). NO was measured by the oxyhemoglobin assay. The influence of SOD, pretreatment of the rats with dexamethasone, as well as kinetic parameters were determined. Type 3 compounds, therefore, are a new class of NO donors. Type 4 and 5 compounds function as their prodrugs.
Syntheses of Novel 3‐Amino‐2(1H)‐thioxo‐4(3H)‐quinazolinones and Evaluation of Their Immunotropic Activity. Part III
Authors: Nawrocka Wanda , Zimecki Michal 
Published: October 2006

AbstractThe synthesis of two series of derivatives containing the quinazolinone‐4 moiety is described. 3‐Amino‐2(1H)‐thioxo‐4(3H)‐quinazolinone (1) was subjected to reactions with halogenoketones and halogenoaldehydes, leading to the production of the corresponding ketones, aldehydes, Schiff bases, and 6‐oxo‐1,4,5‐thiadiazin[2,3‐b]quinazoline derivatives. Subsequently, 1 was condensed with selected α,β‐unsaturated carbonyl compounds, aldehydes, ketones, acid chlorides, and esters. The compounds were tested for their potential activity in a model of humoral and cellular immune response. The tests showed that the compounds exhibited differential immunotropic activities. Of particular interest is compound 19, exhibiting a strong stimulatory activity with regard to cellular immune response and compound 16 exerting a strong inhibitory action in both types of the immune response.
Über die Geburtswehen einer quantifizierenden Ökologie — der Streit um die Kieler Planktonexpedition von 1889
Authors: Breidbach Olaf 
Published: October 2006

AbstractIn 1889 the Kiel plancton expedition started to perform the first quantitative analysis in marine ecology. The methods performed by this expedition caused an extensive discussion about the suitability of quantitative methods in a study of biological organizations. This discussion outlined the theoretical differences between the two main German schools in zoology: the descriptive morphology as performed by Ernst Haeckel and the analytical physiology as initiated by Emil DuBois‐Reymond. The present study describes the positions of both, the morphology and the physiology, one the one hand, to analyze the theoretical background of the new formed ecological science, and on the other hand, to outline some aspects of the principal situation of the German biology in the late 19th century. These more principal aspects are so more of interest as the discussion initiated by the Kiel plancton expedition extended to a controversy about the theoretical value of the theory of evolution. Implications for the theoretical basis of recent ecology are discussed.
De piscibus et aquatilibus libelli III novi (Zürich 1556) Ein bisher unbeachtetes zoologisches Werk von Conrad Gesner
Authors: Bäumer Änne 
Published: October 2006

AbstractConrad Gesner was one of the main representatives of Renaissance‐Humanism. Although having great respect for the knowledge handed down by classical antiquity, he combined his studies of the ancient authors with empirical knowledge obtained by immediate observation of nature. His most famous work was the great „Historia animalium”︁, a comprehense encyclopedia of zoology. Preparing this main zoological work Gesner wrote a small book about fishes „De piscibus et aquatilibus libri III novi”︁ (1556), through which it is possible to gain a deep insight into Gesner's preparatory work and method.
Zwischen Wirtschaft und Wissenschaft — die deutsche Schutzgebiets‐Botanik
Authors: Zepernick Bernhard 
Published: October 2006

AbstractAfter the German Empire was founded in 1871 and, in the following years, had obtained colonies an intensive exploration of these territories began. This fact had two reasons: firstly the government as well as business circles were interested in the results of the research and secondly the development of these territories facilitated essentially the exploration of the flora and vegetation and the research in cultivated plants. The impulse for the research came partly from the government, partly from business circles, partly from scientific societies or from individuals. As a governmental institution the Botanical Research Centre for the German Colonies (Botanische Zentralstelle für die deutschen Kolonien) and as an economic institution the Colonial Economic Committee (Kolonial‐Wirtschaftliches Komitee) were founded in Berlin. Governmental botanical research institutes were founded in the colonies, especially the Research Institute for Land Improvement (Versuchsanstalt für Landeskultur) at Victoria (the Cameroons) and the Biological Agricultural Institute (Biologisch‐Landwirtschaftliches Institut) at Amani (German East Africa). At the end of World War I Germany had lost its colonies. But nevertheless Germans still take part in the botanical exploration of the former colonial territories and in the international efforts at protection of its plant world.