bluuebunny/crossref_metadata_2025 huggingface dataset:
Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, Part 33 From Tetradecane‐ to Octacosanediamines
Authors: Rehse Klaus , Nolte‐Driller Rafaela
Published: October 2006

Twenty alkanediamines were designed according to structure‐activity relationships drawn from previous parts of this series and synthesized. Their general structure is CH3‐(CH2)n‐CHNH2‐(CH2)m‐CHNH2‐(CH2)n‐CH3, (n = 2–10; m = 3–6). Twelve of them inhibited the aggregation of human blood platelets in concentrations between 3–10 μmol/L halfmaximally (Born test, inducer collagen). With increasing m a decreasing n is necessary to achieve the optimum activity. In the most active compounds (7b, 7e, 7p) it is found that m + n = 9. When the nitrogen functions are hydroxyalkylated secondary amines with similar antiplatelet effects are obtained. The conversion of the amino groups into sydnonimines is accompanied by the loss of activity. The bisethoxycarbonylderivatives of 7f and 7m (8f, 8m) exhibited antithrombotic effects in rats after oral administration.
Inhibition of Type 4 Cyclic Nucleotide Phosphodiesterase by 8‐Chloroxanthines
Authors: Arch Jonathan R. S. , Buckle Derek R. , Connolly Brendan J. , Faller Andrew , Fenwick Ashley E. , Murray Kenneth J. , Rami Harshad K. , Smallridge Mark S. , Smith David G.
Published: October 2006

In an endeavour to develop isoenzyme selective inhibitors of the cyclic nucleotide phosphodiesterases, structural modifications of 8‐amino‐1,3‐bis(cyclopropylmethyl)xanthine (BRL 61063) have been investigated. Particularly significant was the observation that certain 7‐aralkyl derivatives incorporating chlorine or bromine in place of the 8‐amino substituent afforded selective inhibitors of the PDE 4 isoenzyme. The 7‐(2‐naphthylmethyl) derivatives of 8‐chloroxanthine 16 and 8‐bromoxanthine 17 in particular showed sub‐micromolar IC50 values against PDE 4 while eliciting some 10 and 100‐fold or greater selectivity, respectively, against the 1b, 1c, 2, 3, and 5a isoenzymes.
Synthesis and Antiplatelet Activity of 1‐tert‐Butylamino‐3‐(3‐thienyloxy)‐2‐propanols
Authors: Abdallah Susana , Darias Victoriano , Donoso Rosa , de Urríes Pilar Jordán , Lissavetzky Jaime
Published: October 2006

The synthesis of new 1‐tert‐butylamino‐3‐(3‐thienyloxy)‐2‐propanols by two alternative methods is described. Their initial antiplatelet activity evaluation against ADP, adrenaline, and collagen is reported, and the preliminary structure‐activity relationships are established. The appropriateness of further pharmacological investigations, especially for the best compound of the series 1f, is indicated.
Stability of Suramin in Aqueous Solution; Possible Implications for the Search for Suramin Metabolites in Patients
Authors: Kassack Matthias , Nickel Peter
Published: October 2006

The stability of an aqueous solution of suramin has been determined. The only degradation product detectable by HPLC was the amine precursor 2. The decomposition kinetics of suramin at different temperatures are shown. Because of first order kinetics the Arrhenius equation could be used to evaluate the decomposition data. A good correlation was obtained between the reaction constants and the temperature (r = 0.9898). After 42 days at 37 °C, 2% of suramin are hydrolysed. Possible implications of our results for the search for suramin metabolites in patients are discussed.
Non‐Steroidal Anti‐Inflammatory Agents, Part 20 [1] Method for Testing Non‐Steroidal Anti‐Inflammatories: The Modified Hen's Egg Chorioallantoic Membrane Test (HET‐CAM Test) Compared to Other Procedures
Authors: Dannhardt Gerd , Kreher Mareta , Nowe Ulrike , Pies Andreas
Published: October 2006

The delay of onset of irritation phenomena at the chorioallantoic membrane of incubated hen's eggs, a parameter for anti‐inflammatory activity, was determined for the pharmaceutical substances diclofenac, flufenamic acid, ibuprofen, indomethacin, ketoprofen, piroxicam, phenylbutazone, salicylic acid, and sodium salicylate. Alongside questions relating to the dose‐effect ratio, metabolisation, recovery, and diffusion of the substances to their site of action were investigated. The reproducibility of the procedure and its selectivity with regard to substances with a different mechanism of action is proven. The method allows classification of the substances according to their anti‐inflammatory potency. However, correlation with the results of enzyme inhibition or in vivo results is only possible to a limited extent.
Synthesis and Pharmacological Studies of 3‐Amino‐2‐methyl‐1‐phenylpropanones as Hypolipidemic Agents in Rodents
Authors: Huang Yunsheng , Hall Iris H.
Published: October 2006

A series of 3‐amino‐2‐methyl‐1‐phenylpropanones were synthesized and proven to have potent hypolipidemic activity in rodents by lowering both serum cholesterol and triglyceride levels at 8 mg/kg/day, i.p. and orally. Many of these analogs showed significantly higher activity than standard drugs, lovastatin and clofibrate at their therapeutic doses. 2‐Methyl‐3‐(perhydroazepin‐1‐yl)‐1‐phenylpropanone (@!4), 3‐(4‐methylpiperazin‐1‐yl)‐1‐phenylpropanone (5), and 2‐methyl‐3‐(4‐pyrrolidinocarbonyl‐methylpiperazin‐1‐yl)‐1‐(4‐fluorophenyl) propanone (17) showed the best overall activities in lowering both serum cholesterol and triglyceride levels in CF1 mice at 8 mg/kg/day after 16 days of treatment. Compounds 4, 5, and 17 lowered serum cholesterol levels 63%, 58%, and 42%, respectively, after 16 days at 8 mg/kg/day i.p. These agents reduced the serum triglyceride levels by 33%, 37%, and 54%, respectively. In Sprague‐Dawley rats these compounds also demonstrated significant serum lipid lowering effects by decreasing both serum cholesterol and triglyceride levels after 14 days of oral drug administration at 8 mg/kg/day. Compound 17 reduced the rat aorta cholesterol levels by 37%, triglyceride levels by 50%, and neutral lipid levels by 34% after 14 days of oral administration. These compounds lowered the chylomicron, VLDL, and LDL cholesterol and triglyceride levels while elevating the HDL cholesterol levels significantly. In hyperlipidemic rodents, these analogs also demonstrated significant serum lipid lowering effects but were less active than in normalipidemic rodents. The activities of some enzymes, such as mouse hepatic acetyl CoA synthetase, HMG CoA reductase, phosphatidylate phosphohydrolase, and hepatic lipoprotein lipase, were significantly reduced by these compounds.
Synthesis and Calcium Antagonistic Activity of 8‐[N‐[2‐(3,4‐Dimethoxyphenyl)ethyl]‐β‐alanyl]‐5,6,7,8‐tetrahydrothieno[3,2‐b][1,4]thiazepine Fumarate
Authors: Erker Thomas , Laimer Ingrid , Huck Sigismund , Boehm Stefan , Studenik Christian , Heistracher Peter
Published: October 2006

KT‐362 is an antiarrhythmic and antihypertensive agent with vasodilating activity. Since it carries a homoveratryl group in the side chain, an obvious relation exists to the verapamil‐type calcium antagonists. Replacement of the fused aromatic moiety in KT‐362 with thiophene provided 8‐[N‐[2‐(3,4‐dimethoxyphenyl)ethyl]‐β‐analyl]‐5,6,7,8‐tetrahydrothieno[3,2‐b][1,4] thiazepine (1). Compound 1 shows a negative chronotropic activity in spontaneously beating right atria (IC50 = 23 μM, n = 7), and a negative inotropic effect in papillary muscles (IC50 = 2.7 μM, n = 7) and left atria (IC50 = 4 μM, n = 6) of the guinea‐pig heart. The decrease of contractility in papillary muscles could be antagonized by increasing the extracellular calcium concentration. Compound 1 was found to affect high (IC50: 70 ± 5 μM) and low (IC50: 129 ± 34 μM) voltage‐activated calcium channel currents as well as voltage‐activated sodium channel currents (IC50: 80 ± 13 μM) in chick dorsal root ganglion neurons. In addition, nicotine‐induced currents were potently inhibited (IC50: 6 ± 0.7 μM) in bovine chromaffin cells.
Phenylamino‐Pyrimidine (PAP) Derivatives: A New Class of Potent and Selective Inhibitors of Protein Kinase C (PKC)
Authors: Zimmermann Jürg , Caravatti Giorgio , Mett Helmut , Meyer Thomas , Müller Marcel , Lydon Nicholas B. , Fabbro Doriano
Published: October 2006

Phenylamino‐pyrimidines represent a novel class of inhibitors of the protein kinase C with a high degree of selectivity versus other serine/threonine and tyrosine kinases. Steady state kinetic analysis of N‐(3‐[1‐imidazolyl]‐phenyl)‐4‐(3‐pyridyl)‐2‐pyrimidinamine (5), which showed potent inhibitory activity, revealed competitive kinetics relative to ATP. The adjacent H‐bond acceptor of the pyrimidine moiety next to an H‐bond donor of the phenylamine was found to be crucial for inhibitory activity. N‐(3‐Nitro‐phenyl)‐4‐(3‐pyridyl)‐2‐pyrimidinamine (7) preferentially inhibited PKC‐α (IC50 = 0.79 μM) and not the other subtypes tested. The inhibition constants of PKC‐α and the antiproliferative effect on T24 human bladder carcinoma cells showed a qualitative correlation, although with some exceptions.
Research on Antifungal and Antimycobacterial Agents. Synthesis and Activity of 4‐Alkylthiopyridine‐2‐carbothioamides
Authors: Klimešová Vera , Svoboda Martin , Waisser Karel , Machácek Miloš , Buchta Vladimír , Odlerová Želmíra
Published: October 2006

A series of 4‐alkylthiopyridine‐2‐carbothioamides have been prepared and evaluated in vitro for antimicrobial activity. Chemical structures have been demonstrated by IR and 1H NMR data and by elemental analysis. The antimycobacterial activity of these compounds against Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium, and Mycobacterium fortuitum, and the antifungal activity against Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, Trichosporon beigelii, Trichophyton mentagrophytes, Aspergillus fumigatus, and Absidia corymbifera were determined by the MIC values. Compounds 3 exhibit good antimycobacterial activity compared to isoniazide. A moderate antifungal activity was observed against T. mentagrophytes. Activity is influenced by hydrophobicity of the alkyl group.
Structure‐Activity Relationship Studies of CNS Agents, Part 31[1]: Analogs of MP 3022 with a Different Number of Nitrogen Atoms in the Heteroaromatic Fragment — New 5‐HT1A Receptor Ligands
Authors: Paluchowska Maria H. , Dereń‐Wesońek Anna , Mokrosz (deceased) Jerzy L. , Charakchieva‐Minol Sijka , Chojnacka‐Wójcik Ewa
Published: October 2006

Two series of new MP 3022 analogs, i.e. 1‐(o‐methoxyphenyl)‐4‐n‐propylpiperazines (3, 4a, 4b, 6–9, and 12–13) and 2‐(n‐propyl)‐1,2,3,4‐tetrahydroisoquinolines (5a, 5b, 11a, and 11b) containing a terminal heteroaromatic system with a different number of nitrogen atoms, were synthesized and their 5‐HT1A/5‐HT2A and α1 receptor affinity was assayed. The majority of investigated piperazines may be classified as non‐selective 5‐HT1A/5‐HT2A/α1 receptor ligands. Compounds 3, 4a, 4b, 7–9a with the highest affinity for 5‐HT1A receptors (Ki = 4–54 nM) were tested in vivo. Their functional activity was differentiated; while 3, 8, and 9a behaved like weak antagonists of postsynaptic 5‐HT1A receptors, 4b and 7 may be classified as potential partial 5‐HT1A receptor agonists. Isomer 4a has characteristic features of a potential weak postsynaptic 5‐HT1A receptor agonist.
New NO‐Donors with Antithrombotic and Vasodilating Activities, Part 14 1,3,4‐Triazol‐1‐oles
Authors: Rehse Klaus , Piechocki Daniela , Schober Markus , Scheffler Heike , Reitner Nora , Unsöld E.
Published: October 2006

Five 1,3,4‐triazol‐1‐oles (5a—f) with different alkyl, aryl, and arylalkyl substituents in 2,5‐position were synthesized and tested for their antithrombotic properties. The 2,5‐dimethyl derivative 5a was most active. 2 h after administration of 60 mg/kg to rats thrombus formation by a laser beam was inhibited by 42 % in arterioles and by 33 % in venules. At the same dose the blood pressure of SHR rats was slightly (5%) but significantly decreased even 4 h after application of 5a. This pattern of activities suggests a nitric oxide mediated mechanism of action.

1,1′‐Azo‐bis‐ethanone oxime (7) — the synthetic precursor of 5a — inhibited the aggregation of blood platelet (Born test) with an IC50 = 15 μmol/L.
Asymmetric Synthesis and Structure‐Activity Relationship of the Four Stereoisomers of the Antibiotic Amidinomycin Part 2: Microbiological Testing
Authors: Sung Sun‐Young , Kist Manfred , Frahm August W.
Published: October 2006

The stereoisomers of amidinomycin 7 and their intermediates 1–6, which are produced from homochiral 3‐oxocyclopentanecarboxylic acids by asymmetric synthesis, are tested for their antimicrobial effects by agar diffusion test and by Bouillon serial dilution assay. Their antibiotic activities against Bacillus subtilis, Staphylococcus aureus, and Micrococcus luteus, respectively, are reported. Structure‐activity relationships depend on the type and combination of functional groups, on only the relative stereochemistry as well as on the grade of lipophilia of the tested compounds.
Synthesis and Dopaminergic Properties of 3‐ and 4‐Substituted 1‐{2‐[5‐(1H‐Benzimidazole‐2‐thione)]ethyl}piperidines and Related Compounds
Authors: Dukic Sladjana , Kostic‐Rajacic Sladjana , Šoškic Vukic , Joksimovic Jelena
Published: October 2006

With an aim of creating new, high affinity dopaminergic ligands, six different 3‐ and 4‐substituted 1‐{2‐[5‐(1H‐benzimidazole‐2‐thione)]ethyl}piperidines and nine related heterocyclic congeners were synthesized and evaluated for in vitro binding affinity at D1 and D2 dopamine receptors. Synaptosomal membranes prepared from fresh bovine caudate nuclei were used as a source of the dopamine receptors. Only 4‐[bis‐(4‐fluorophenyl)methylene]‐piperidines, compounds 9e, 10d, and 11d, expressed moderate affinity for the D1 receptors, while all other compounds were inactive competitors of [3H]SCH 23390. Compounds 9c, 9d, 10c, 11a, and 11c were inactive in the D2 receptor binding assay, as well. Derivatives of 4‐phenylpiperidine (9–11b) and 3‐phenyl‐piperidine (10a) expressed a moderate to low affinity for the D2 receptors. However, racemic (±)‐1‐{2‐[5‐(1H‐benzimidazole‐2‐thione)]ethyl}‐3‐phenylpiperidine 9a and its enantiomer (+)‐9a behaved as selective, high affinity D2 receptor ligands, the latter being some four times more active than the racemate.
Synthesis and Cytotoxic Action of 3,5‐Isoxazolidinediones and 2‐Isoxazolin‐5‐ones in Murine and Human Tumors
Authors: Hall Iris H. , Izydore Robert A. , Zhou Xaioming , Daniels Dwayne L. , Woodard Tyrone , Debnath Manik L. , Tse Elaine , Muhammad Rosallah A.
Published: October 2006

The 3,5‐isoxazolidinediones and 2‐isoxazolin‐5‐ones demonstrated potent cytotoxicity against the growth of human Tmolt3 T cell leukemia, murine P388 and L1210 leukemias, as well as human HeLa‐S3 uterine carcinoma and glioma tumor cell growth. The specificity of the 3,5‐isoxazolidinedione and 2‐isoxazoline‐5‐one derivatives as cytotoxic agents varied with the histological type of tumor cell. Selected compounds were active against solid HeLa uterine, KB nasopharynx, skin A431, SW‐480 adenocarcinoma, osteosarcoma and glioma growth. Selected compounds demonstrated in vivo antineoplastic activity against Ehrlich ascites carcinoma growth. In L‐1210 leukemia cells, the agents blocked DNA and protein synthesis at 25,50 and 100 μM over 60 min. The agents were effective in reducing rate limiting enzymes in the de novo purine and pyrimidine pathways. In addition they suppressed dihydrofolate reductase and ribonucleoside reductase activities with moderate inhibition of DNA and RNA polymerase activities. DNA itself was not a target of the agents.
Influence of Various Estrogens on Biotransformation: Affinity to Cytochrome P‐450, Structure Activity Relationships, and Scavenger Function
Authors: Gernhardt Sabine , Karge Elke , Schönecker Bruno , Klinger Wolfgang
Published: October 2006

Nine natural and synthetic estrogens, all derived from endogenous 17β‐estradiol, were tested for their affinity to cytochrome P‐450 (P450). Binding spectra of the estrogens with rat liver microsomal P450 and inhibition kinetics with characteristic monooxygenase model reactions (ethylmorphine N‐demethylation, EN, and ethoxycoumarin O‐deethylation, EO) were determined. In addition, uncoupling effects and/or free radical scavenger functions were analysed by NADPH/Fe++ stimulated microsomal luminol‐and lucigenin‐amplified chemiluminescense (CL). 17β‐Estradiol, 17α‐ethynylestradiol, and D‐estradiol 3‐methyl ether inhibited both monooxygenase reactions of cytochrome P‐450, whereas L‐estradiol 3‐methyl ether inhibited EO only. 17β‐Estradiol, 17α‐ethynylestradiol, and D‐estradiol 3‐methyl ether seem to act as free radical scavengers. From the results both structure activity relationships could be established and data on possible interferences with drug metabolism obtained. The enantiomers D‐ and L‐estradiol 3‐methyl ether differ in their effects on these systems.
Synthesis and Calcium Channel Modulating Effects of Isopropyl 1,4‐Dihydro‐2,6‐dimethyl‐3‐nitro‐4‐(thienyl)‐5‐pyridinecarboxylates
Authors: Miri Ramin , Howlett Susan E. , Knaus Edward E.
Published: October 2006

A group of racemic isopropyl 1,4‐dihydro‐2,6‐dimethyl‐3‐nitro‐4‐(thienyl)‐5‐pyridinecarboxylates 7a–f were prepared using a modified Hantzsch reaction that involved the condensation of a thienylcarboxaldehyde 4a–f with isopropyl 3‐aminocrotonate 5 and nitroacetone 6. In vitro calcium channel antagonist activities were determined using a guinea pig ileum longitudinal smooth muscle (GPILSM) assay. Compounds 7a–f exhibited weaker calcium channel antagonist activity (IC50 = 10−5 to 10−7 M range) than the reference drug nifedipine (IC50 = 1.43 × 10−8 M). The point of attachment of the C‐4 thienyl ring system was a determinant of antagonist activity [3‐thienyl (7b) > 2‐thienyl (7a)]. A 5‐substituent in the 2‐thienyl moiety influenced antagonist activity where the potency order was 5‐bromo‐2‐thienyl 7f ≥ 5‐methyl‐2‐thienyl 7c > 2‐thienyl 7a. Although the 5‐methyl‐2‐thienyl 7c and 3‐methyl‐2‐thienyl 7d isomers are equipotent antagonists, the 5‐bromo‐2‐thienyl compound 7f appears to be marginally more active than the 4‐bromo‐2‐thienyl isomer 7e. The 2‐thienyl compound 7a, unlike the 3‐thienyl isomer 7b, exhibited an agonist effect on GPILSM in the absence of the muscarinic agonist carbachol. Effects of the 2‐thienyl 7a and 3‐thienyl 7b isomers on the magnitude of calcium current were determined in guinea pig ventricular myocytes with voltage clamp techniques. Results showed that 2‐thienyl 7a inhibited calcium current (antagonist) when voltage steps were made from a potential of ‐40 mV. However, when voltage steps were made from ‐60 mV, 7a enhanced calcium current (agonist). The 3‐thienyl isomer 7b had little, if any, effect on calcium current.
An Improved Synthesis of the Anti‐Picornavirus Flavone 3‐O‐Methylquercetin
Authors: Boers Frank , Deng Bo‐Liang , Lemière Guy , Lepoivre Jozef , De Groot Alex , Dommisse Roger , Vlietinck Arnold J.
Published: October 2006

Two optimised procedures to synthesise 3‐O‐methylquercetin (1), an important antivirally active flavone, are presented: one is based on an Allan‐Robinson condensation, the other one on a modified phase transfer catalysed Baker‐ Venkataraman transformation.
Synthesis and Neuropeptide Y Y1 Receptor Antagonistic Activity of N,N‐Disubstituted ω‐Guanidino‐ and ω‐Aminoalkanoic Acid Amides
Authors: Müller Manfred , Knieps Sebastian , Geßele Karin , Dove Stefan , Bernhardt Günther , Buschauer Armin
Published: October 2006

Potent arpromidine‐type histamine H2 receptor agonists such as BU‐E‐76 (He 90481) were among the first non‐peptides reported to display weak neuropeptide Y (NPY) Y1 receptor antagonist activity. In search of new chemical leads for the development of more potent NPY antagonists, a series of N,N‐disubstituted ω‐guanidino and ω‐aminoalkanoic acid amides were synthesized on the basis of structure‐activity relationships and molecular modeling studies of arpromidine and related imidazolylpropylguanidines. In one group of compounds the imidazole ring was retained whereas in the second group it was replaced with a phenol group representing a putative mimic of Tyr36 in NPY. Although the substitution patterns have not yet been optimized, the title compounds are NPY Y1 antagonists in human erythroleukemia (HEL) cells (Ca2+ assay) achieving pKB values in the range of 6.3–6.6. For representative new substances tested in the isolated guinea pig right atrium histamine H2 receptor agonism could not be found. In the N‐(diphenylalkyl)amide series, compounds with a trimethylene chain were more active Y1 antagonists than the ethylene homologs. Concerning the spacer in the ω‐amino or ω‐guanidinoalkanoyl portion, the best activity was found in compounds with a four‐ or five‐membered alkyl chain or a 1,4‐cyclohexylene group. Surprisingly, in contrast to the phenol series, in the imidazole series the compounds with a side chain amino group turned out to be considerably more potent than the corresponding strongly basic guanidines. Thus, the structure‐activity relationships appear to be different for the diphenylalkylamide NPY antagonists with one or two basic groups.
Determination of Fluoride Impurities in Calcium Ascorbate Comparison of Gas Chromatography and Ion Selective Electrode Potentiometry
Authors: Yuwono Mochammad , Ebel Siegfried
Published: October 2006

Fluoride impurities in pharmaceutical grade calcium ascorbate were determined analytically by capillary gas chromatography (GC) and ion‐selective electrode potentiometry (ISE). In the GC method, the amount of fluoride impurities was quantitatively analyzed following the conversion of fluoride to its corresponding trimethylsilane derivative using trimethylchlorsilane. The derivatization procedure was performed under acidic conditions and the generated trimethylfluorsilane was subsequently extracted with n‐hexane prior to GC analysis using isopentane as an internal standard.

In the potentiometric method, the fluoride content was determined by relating the potential of the sample solution at different concentrations to a calibration curve. A comparative evaluation between the two methods was validated according to their linearity, precision, and accuracy. The fluoride concentrations found by means of GC and ISE were (0.94 ± 0.04) ppm and (0.85 ± 0.12) ppm, respectively. The student's t‐test (error of the first kind α = 0.1) indicated that there was no significant difference between the results obtained by the two methods.
Problems in using birth certificate files in the capture‐recapture model to estimate the completeness of case ascertainment in a population‐based birth defects registry in New York State
Authors: Wang Ying , Druschel Charlotte M. , Cross Philip K. , Hwang Syni‐An , Gensburg Lenore J.
Published: October 2006

BACKGROUND: The limitations and underlying assumptions of the capture‐recapture methods have hindered their application in epidemiological settings, especially in evaluating the completeness of birth defects registries. This study explored the possibility of using birth certificates as the secondary data source in a simple two‐source capture‐recapture model to estimate the completeness of case ascertainment of the Congenital Malformations Registry (CMR) for selected major birth defects. METHODS: The CMR and the birth certificates were used as the primary and secondary sources, respectively. Children who were born in 1996–2001 and had selected major birth defects were identified from the two sources. The accuracy of the diagnoses was examined by comparing the individual birth defect categories of the children from the two sources. RESULTS: Discrepancies in birth defect categories in the two data sources and false positives in the birth certificates were the major problems encountered in estimating the completeness of the CMR using the simple two‐source capture‐recapture method. The estimated completeness for selected major birth defects was only about 71%. Stratified analyses resulted in relatively high estimated completeness for oral clefts (90%) and Down syndrome (88%). CONCLUSIONS Although the birth certificate data was not a good source for estimating the completeness of case ascertainment of the CMR using capture‐recapture methods, the analyses provided reasonable estimates for some conditions that were relatively easy to identify and diagnose at birth, such as oral clefts and Down syndrome. Birth Defects Research (Part A), 2006. © 2006 Wiley‐Liss, Inc.
Inter‐rater agreement of assessed prenatal maternal occupational exposures to lead
Authors: Correa Adolfo , Min Yuan‐I , Stewart Patricia Ann , Lees Peter S. J. , Breysse Patrick , Dosemeci Mustafa , Jackson Leila W.
Published: October 2006

BACKGROUND: Industrial hygienists' assessments of prenatal occupational exposures based on parental job histories is a promising approach for population‐based case‐control studies of birth defects and other perinatal outcomes. However, evaluations of inter‐rater agreement of such assessments have been limited. METHODS: We examined inter‐rater agreement of occupational lead exposure assessments of maternal job reports by industrial hygienists in a population‐based case‐control study of parental occupational lead exposure and low birth weight. A total of 178 jobs with potential exposure to lead during the 6 months before pregnancy to the end of pregnancy were examined. Three industrial hygienists evaluated these jobs independently for exposure to lead including probability of exposure, type of exposure, route of entry, exposure frequency, duration, and intensity. Inter‐rater agreement of these assessments beyond chance was evaluated using the kappa statistic (κ). RESULTS: In general, inter‐rater agreement was greater for assessment of direct exposures than assessment of indirect exposures. However, inter‐rater agreement varied with the lead exposure metric under consideration, being: 1) fair to good for type of direct exposure (i.e., inorganic or organic), respiratory exposure and frequency of exposure to direct inorganic lead, hours per day of direct (i.e., inorganic or organic), and intensity of direct inorganic exposure; 2) poor for probability and type of indirect exposure (inorganic or organic); and 3) indeterminate for frequency of direct organic exposure, frequency of indirect exposures (organic or inorganic), and intensity of direct exposures (organic or inorganic). CONCLUSION: Retrospective assessment of maternal prenatal exposures to lead by industrial hygienists can provide some reliable metrics of exposure for studies of perinatal outcomes. Reliability studies of such exposure assessments may be useful for: quantifying the reliability of derived exposure metrics; identifying exposure metrics for exposure‐outcome analyses; and determining the reliability of prenatal occupational exposures to other agents of interest. Birth Defects Research (Part A), 2006. © 2006 Wiley‐Liss, Inc.
Mathematik und Religion in der frühen Neuzeit
Authors: Breger Herbert
Published: October 2006

Some protestant Mathematicians had a strong preoccupation with the Day of Judgement. Stifel, Faulhaber, Napier and Newton made calculations in order to determine the date of the end of the world. Craig gave mathematical rules for a decline in the reliability of Christian tradition; in order to prevent a reliability of nearly zero, the Day of Judgement must come before. Furthermore, some conflicts between theology and mathematics are discussed. The Council of Konstanz condemned Wyclif's theory of the continuum. It seems that the relation between part and whole was a crucial point between the Aristotelians and the “moderns”.
Akzentverschiebung ‐ Zur Geschichte der Semitistik und Islamwissenschaft während des ‚Dritten Reichs’︁
Authors: Hanisch Ludmila
Published: October 2006

Fifty years after World War II the history of Semitic and Islamic Studies during the period of nazism has more or less remained ‘terra incognita’. The article shows that academic activities in this field did not remain uninfluenced by that period. In addition to the banishment of Jewish scholars, a concentration on Arabian Studies took place and scholars contributed for the weltanschauung of the Third Reich. To date not all the outcomes can be presented. Yet, one of them is easily observable: The study of Jewish religion, history and culture became a special branch, it is no longer part of Oriental studies.
Bewertung durch Auswahl Wieviel wählt der Wissenschaftshistoriker aus, wieviel übergeht er?
Authors: Graf‐Stuhlhofer Franz
Published: October 2006

In presenting events in history, the historian is forced to select a few people. This selection of people choosen by the historian is an evaluation in itself. How restricted is his selection? In the history of science we could ask: How large is the proportion of selected scientists in comparison with those that are not mentioned? The answer: A book that covers the entire history of science, usually will select one out of about three hundred scientists.
Waffenentwicklung – Normsetzungen für den Krieg
Authors: Messerschmidt Manfred
Published: October 2006

Armament Development – Warfare Rules. Modern armament technology was discussed at the Hague Conferences in 1899/1907. Air war was seen already as a coming danger. Nevertheless, the big powers could not reach a specific agreement on air war. There was only a provisional five years' rule not to drop explosives from aircraft. In 1907 the powers did not prolong this rule. The question was, therefore, whether Articles 25 and 27 of the Hague Convention on land warfare as well as the Marten's Clause (Preamble to the Hague Convention) were to be applied to air warfare.

During World War I the powers neglected these rules by referring to the ‚legal justification’︁ of achieving the goals of war and of the right of reprisals. The inter‐war years did not see better results. Attempts made at the Washington Conference of 1921/22 to reach an agreement resulted only in the proposals made in 1923 by the Hague Commission of Jurists. No agreement was made between the wars. The military, air‐war planners and industrials hardly even discussed the conflicting relationship between air warfare and international law. Discussions, war games, strategic thought and armaments envisaged area‐bombardment directed against the morale of the population. World War II implemented this kind of war on a great scale. Similar developments took place with respect to chemical warfare. It was only fear of reprisals that prevented gas‐air war. Both kinds of war chemical warfare in World War I and strategic air war directed against non‐combatants in World War II had not been in accordance with the Hague Convention and with general rules of international law.
Soziobiologische Kriegführung? Der Generalplan Ost
Authors: Schleiermacher Sabine
Published: October 2006

In studying the genesis of ‚Generalplan Ost’︁ one can elucidate the alliance of academic research and military expansion in Nazi Germany in a unique way. By ‚Generalplan Ost’︁ we understand the total German planning effort in transforming the territories of Poland, the Baltic republics and Soviet Union, which were occupied since the beginning of World War II. In this scientists were not only provided with ample opportunities for research by the National Socialist government, but the Nazi policy of occupation created the preconditions necessary for putting theoretical models into practice. This was done in complete disregard of pre‐existing structures in population, settlement, society, economy, and patterns of traffic. The principal aim consisted in the total transformation of the envisaged Eastern European sphere and the implantation of a new National Socialist social order style in Eastern Europe. Scientific planning not only implied a declaration of war against the very people living in the geographic sphere covered by the plan, but presupposed the existence of war in order to put the plan into practice. In a rare mixture of social science, geography and biology, instruments of science made possible and provoked the social selection and deportation of human beings as well as attempts at Germanization and ‚Umvolkung’︁. It is a well known fact, that deportation and extermination became a brutal reality as an intrinsic ingredient of these planning efforts.
Georges Canguilhem als Medizinhistoriker
Authors: Grond‐Ginsbach Caspar
Published: October 2006

The work of the French philosopher Georges Canguilhem is introduced here. Medical historiography is not the ultimate aim of Canguilhems work, but rather a tool for the analysis ef epistemological questions. These questions are to be investigated, as well as the art of medical history that Canguilhem considers to be helpful for such investigations. French „epistemology”︁, a direction of philosophy of science to which Canguilhem belongs, is discussed first. Canguilhem's epistomology does not aim at a rational reconstruction of decontextualized scientific results, but at an historical reconstruction of science. It analyses the functioning of scientific concepts in relation of their historical context. The main themes of Canguilhems work (biological normality, scientific ideology and history of physiology) are summarized in a second part of this study. Finally we investigate the importance of Canguilhem for modern research in history of medicine.
„Die gesamte Philosophie ist eine Neuerung in alter Unkenntnis”︁ Johannes Keplers Neuorientierung der Astronomie um 1600
Authors: Knobloch Eberhard
Published: October 2006

Johannes Kepler belonged to a long tradition of inquiring into nature with reference to God. This applies to Ptolemy, N. Copernicus, Chr. Clavius. Kepler's „new kind of poem”︁ is analyzed in five sections which are based on Keplerian key words: Innovation, Hypothesis, Cause, Soul, Picture. Kepler consciously adhered to new questions, new answers, new methods. He relied on a new notion of hypothesis. His celestial dynamics included a celestial psychology whereby he used a visual conception of astronomy.
Von der klassischen Trägheit zur dynamischen Raumzeit: Albert Einstein und Ernst Mach
Authors: Renn Jürgen
Published: October 2006

The paper analyzes Einstein's path to the General Relativity in the context of its historical alternatives. The main alternatives were constituted by an exclusively field theoretical approach to gravitation and a generalization of mechanics following suggestions by Ernst Mach. It is shown that Einstein succeeded in avoiding the pitfalls of both approaches by suitably combining them. The characteristics and the success of his path to General Relativity are explained by his non‐specialist, integrative outlook on the problem of classical physics.
Die Johannes Gutenberg‐Universität als ‘Université Rhénane’ Zur Wiedergründung der Mainzer Hochschule 1946 im Kontext der französischen Besatzungspolitik
Authors: Zauner Stefan
Published: October 2006

In the spring of 1946, the French Military Government in occupied Southwest Germany re‐opened the University of Mainz, closed down some 150 years ago. The article places this creation in the overall scheme of French cultural and (re)educational policies in postwar Germany, and describes the formative phase of an academic institution which was supposed to be a counterbalance to traditional German universities, mainly by cultivating a humanist, democratic, and pro‐European spirit, but also by introducing new institutional structures, educational units, and recruitment patterns. The author argues that ambitious claims and harsh reality differed considerably, and that the concurrence of various and complex crisis phenomena led to an early “normalization” of the would‐be francophile paragon.
Die kernphysikalischen Ambitionen des Reichspostministers Ohnesorge
Authors: Stange Thomas
Published: October 2006

While the history of the German uranium project during the Second World War has been described in much detail, the funding of nuclear research by the Minister of the Reichspost, Wilhelm Ohnesorge, has found but little attention. The reasons for this were presumably the relative scarcity of documents and an underestimation of the efforts made and the results achieved by the research branch of the Reichspost, the Reichspostforschungsanstalt. The essay attempts to fill this gap in describing how and why Ohnesorge became interested in nuclear physics, how two institutes were set up, and what their objectives were.
Wisse die Wege! Hildegard von Bingen zum 900. Geburtstag
Authors: Bäumer‐Schleinkofer Änne
Published: October 2006

»Know the Ways!« On the occasion of Hildegard's of Bingen 900th birthday. Hildegard is regarded as one of the most important women of the Middle Ages. Her contemporaries from all over the world wrote letters to her searching for help and prayer. Universilary working she wrote works about medicine, natural history, compositions of chants for the honour of God and his creation and more than three hundred letters to people all over the world including the popes and the emperor. Hildegard's work and the way she understood herself were strongly marked by vision and prophecy. Her works were of divine origin by vision and audition. Her aim was the religious interpretation of the whole universe and a Christian life in the sense of the bible. Heaven and earth, faith and natural science, medicine and religion, the human existence in all its facts and potentials, everything was a mirror of divine love to her. In her first work Scivias („Know the Ways”︁) she is considering on the history of creation and salvation, from the origin of the world and of man over Christ's salvation to the fulfillment at the end of times. In the centre is standing the human being as microcosm reflecting the whole world in all conditions and laws. Man is the main work of god, reflecting in his doing and thinking God's love. Man has to know the ways that means to live the life of love in all consequences including reproduction by creating a new human being for the praise of God.
Botanische Gärten und Pflanzengeographie als Herrschaftsrepräsentationen
Authors: Klemun Marianne
Published: October 2006

The article deals with different botanical gardens in Vienna. These places of knowledge in the 18th century are constituted to operate science professionally. Different forms of gardens and practices document various opinions of science. Nikolaus J. von Jacquin forms the centre of botany in Vienna. Botanical Travellers have taken plant from all over the world, from the periphery to the centers, the botanical gardens in Europe. Symbolized by collectors the contribution of worldwide plant material is visualised as plant geography in the first map of the distribution of plants.
Wörter und Bilder in der österreichisch‐ungarischen Philosophie: Von Palágyi zu Wittgenstein
Authors: Nyíri Kristóf
Published: October 2006

The thesis according to which technologies of communication have implications not just for the form, but also for the content and indeed for the overall logic of what is being communicated rests on a set of general philosophical assumptions as regards the relation between thought and its medium. The paper shows that formulating these assumptions, and elaborating them, has been a characteristic concern of Austro‐Hungarian philosophy; that between the philosophers who played a role in the relevant endeavours there obtained significant, sometimes mutual, influences; and that Austro‐Hungarian realities ‐ basically, the phenomenon of disturbed communication within the Habsburg Empire ‐ had a marked effect on their thought.
Strukturwandel der Wissenschaft im Nationalsozialismus
Authors: Sieg Ulrich
Published: October 2006

National Socialism brought about profound changes for the German academic system. Forced emigration not just sent outstanding scholars into exile, thus closing down promising research venues. In fact, it changed the entire climate of scientific inquiry by removing intellectual outsiders from the scene, whose absence usually precludes any success of innovative research. In most disciplines this led to a dominance of just a few academic ‘schools’ and paradigms, which severely harmed intra‐discipline accountability and innovation. The academic bureaucracy worked more effectively than has been assumed for a long time: practice‐oriented research enjoyed massive state support, and huge research projects outside the universities flourished. At the same time the National Socialists looked ambivalently at the universities themselves. They savored the legitimizing functions of the arts and sciences, and yet they distrusted the professors as exponents of the bourgeois world of old. Contrary to the blooming sciences such as biology, chemistry, and physics, the arts and humanities had a hard time demonstrating their practical applicability. In order to prove their worth by means of giving advice to the political sphere, they formed interdisciplinary combines, which were massively funded by the ‘Deutsche Forschungsgemeinschaft’. The ‘Deutsche Wissenschaft’, which has been incorrectly marginalized in numerous accounts, served in part to provide a Weltanschauung justification for these networks. While the German academic community in 1945 tried to pick up the threads of the a‐political self‐ understanding of the 1920s, in fact there were numerous continuities to academic life before and after 1945. Among them were the encompassing loss of international contacts, the strengthening of hierarchical structures, and the importance of feasibility criteria for the culture of innovation. The arts and humanities (Geisteswissenschaften) could not regain the lost territory of significance, which they had suffered during the Third Reich. It is mainly their development which showed an amazing persistence of national socialist patterns of view and of concepts of the enemy, which in turn as late as 1968 inspired in part the anti‐bourgeois thrust of the critique of the academic world.
Insight into the free‐radical‐scavenging mechanism of hydroxyl‐substituent Schiff bases in the free‐radical‐induced hemolysis of erythrocytes
Authors: Tang You‐Zhi , Liu Zai‐Qun
Published: October 2006

This work aimed to explore the mechanism by which hydroxyl‐substituent Schiff bases scavenge free‐radicals. Thus, four Schiff bases, that is benzylidene aniline (BAN), 2‐(phenyliminomethyl)phenol (BAH), 4‐benzimidoylphenol (PBH) and 2‐benzimidoylphenol (OBH), were applied to protect human erythrocytes against 2,2′‐azobis(2‐amidinopropane hydrochloride) (AAPH)‐induced hemolysis. The results revealed that the OH attached to the ortho‐position of methylene in Schiff base scavenges 1.46 radicals per molecule, the OH attached to the para‐position of the N atom scavenges 2.94 radicals and the OH attached to the ortho‐position of the N atom scavenges 3.63 radicals. In addition, four Schiff bases were used together with some familiar antioxidants, such as 6‐hydroxyl‐2,5,7,8‐tetramethyl chroman‐2‐carboxylic acid (Trolox), L‐ascorbic acid (VC), α‐tocopherol (TOH) and L‐ascorbyl‐6‐laurate (VC‐12) in AAPH‐induced hemolysis of erythrocytes. It was found that, except for BAN+VC‐12, BAH + VC‐12, OBH + VC‐12 and PBH+TOH, all the other combinations protected erythrocytes more perfectly than when used individually. This result demonstrated that a promotive protection existed between Schiff base and other antioxidants and this improved their ability to scavenge free‐radicals. Finally, IC50 values of the aforementioned Schiff bases together with 2‐((o‐hydroxylphenylimino) methyl)phenol (OSAP) and 2‐((p‐hydroxylphenylimino)methyl)phenol (PSAP) were determined by reaction with two radical species, that is, 2,2′‐azinobis(3‐ethylbenzothiazoline‐6‐sulfonate) radical (ABTS+·) and 2,2′‐diphenyl‐1‐picrylhydrazyl (DPPH). The results implied that the molecular framework of a Schiff base and an OH attached to the ortho‐position of methylene were apt to reduce radicals, but the OH attached to the aniline ring in a Schiff base was prone to scavenge radicals directly. Copyright © 2006 John Wiley & Sons, Ltd.
Triphenylphosphane‐Functionalised Amphiphilic Copolymers: Tailor‐Made Support Materials for the Efficient and Selective Aqueous Two‐Phase Hydroformylation of 1‐Octene
Authors: Bortenschlager Martin , Schöllhorn Nicole , Wittmann Anton , Weberskirch Ralf
Published: October 2006

Amphiphilic copolymers (random P1 and block P2) based on 2‐oxazolines were synthesised with triphenylphosphane ligands covalently linked to the polymers by means of a metal‐free synthesis route. The resulting macroligands were used in the aqueous two‐phase hydroformylation of 1‐octene. The influence of the polymer architecture (random and block copolymers) on activity and selectivity of the hydroformylation reaction was investigated and compared with that of nonfunctionalised copolymers (random P3 and block P4) and RhI/triphenylphosphane trisulfonate as a water‐soluble catalyst. The highest activities were observed for the random copolymer P1 (p=50 bar, T=100 °C, c=8×10−4 mol L−1) with a turnover frequency (TOF) of 3700 h−1, whereas the corresponding block copolymer P2 reached TOF numbers of 1630 h−1. Additionally, both macroligands indicated efficient suppression of isomerisation and led to almost constant n/iso selectivities of about 3 after complete substrate conversion. Copolymers P3 and P4 showed, under identical reaction conditions, strong isomerisation after 40–60 % conversion (n/iso≈0.7) and maximum activities of 1560 h−1 (P3) and 1330 h−1 (P4) at a concentration of 5×10−3 mol L−1.
Preparation and Structure of Mono‐ and Binuclear Half‐Sandwich Iridium, Ruthenium, and Rhodium Carbene Complexes Containing 1,2‐Dichalcogenolao 1,2‐Dicarba‐closo‐Dodecaboranes
Authors: Wang Xin , Liu Shuang , Weng Lin‐Hong , Jin Guo‐Xin
Published: October 2006

The synthesis of half‐sandwich transition metal complexes containing both 1,2‐dichalcogenolato‐1,2‐dicarba‐closo‐docecaborane (CabE,E) [CabE,E=E2C2(B10H10); E = S, Se] and N‐heterocyclic carbene (NHC) ligands is described. Addition of mono‐NHC ligand to the 16e half‐sandwich dichalcogenolato carborane complexes [Cp*Rh(CabE,E)], [Cp*Ir(CabS,S)], [(p‐cymene)Ru(CabS,S)] (Cp* = pentamethylcyclopentadienyl) gives corresponding mononuclear 18e dithiolate complexes of the type [LM(CabE,E)(NHC)]: [Cp*M(CabS,S)(1‐ethenyl‐3‐methylimidazolin‐2‐ylidene)] (M = Ir (2), Rh (3)), [Cp*Rh(CabE,E)(3‐methyl‐1‐picolyimidazolin‐2‐ylidene)] [E = S (6), Se (7)], [(p‐cymene)Ru(CabS,S)(NHC)] [NHC = 1‐ethenyl‐3‐methylimidazolin‐2‐ylidene (4), 3‐methyl‐1‐picolyimidazolin‐2‐ylidene (8)], whereas bis‐NHC give centrosymmetric binuclear complexes [{Cp*M(CabS,S)}2(1,1′‐dimethyl‐3,3′‐methylene(imidazolin‐2‐ylidene))] [M = Rh (10), Ir (11)]. The complexes were characterized by IR, NMR spectroscopy and elemental analysis. In addition, X‐ray structure analyses were performed on complexes 2–4, 6, 8, 10 and 11.
Iron‐Based Layered Superconductor: LaOFeP.
Authors: Kamihara Yoichi , Hiramatsu Hidenori , Hirano Masahiro , Kawamura Ryuto , Yanagi Hiroshi , Kamiya Toshio , Hosono Hideo
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.
Urea Coordinated Titanium Trichloride TiIII[OC(NH)2]6Cl3: A Single Molecular Precursor Yielding Highly Visible Light Responsive TiO2 Nanocrystallites.
Authors: Li Ji‐Guang , Yang Xiaojing , Ishigaki Takamasa
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.
Azidoaurates of the Alkali Metals.
Authors: Afyon Semih , Hoehn Peter , Armbruester Marc , Baranov Alexey , Wagner Frank R. , Somer Mehmet , Kniep Ruediger
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.
Practical by Ligand Design: A New Class of Monodentate Phosphoramidite Ligands for Rhodium‐Catalyzed Enantioselective Hydrogenations.
Authors: Zhao Baoguo , Wang Zheng , Ding Kuiling
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.