摘要:

AbstractThe novel concept of penicillin derivatives4with a medium‐sized instead of a β‐lactam ring is presented. Two synthetic paths were invented, resulting in the evaluation of the synthetic potential in the succinic, glutaric, and adipic acid series. A number of novel penicillin‐derived thiazolidines were prepared, notably the derivatives16and22with anellated 7‐ and 13‐membered l

ISSN:0365-6233    

DOI:10.1002/ardp.19953280302

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe amino/imino equilibrium is studied in free bases and hydrochloride salts of amidinobenzisothiazole derivatives by IR and1H‐NMR spectroscopy. The X‐ray crystallographic analysis of two of these compounds shows that the free base exists as amino form whereas the hydrochloride as imino f

ISSN:0365-6233    

DOI:10.1002/ardp.19953280303

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractVarious aryl 1‐pyrryl sulfones were synthesized and tested as inhibitors of HIV‐1, 2‐Nitrophenyl‐2‐ethoxycarbonyl‐1‐pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. Thein vitroanti‐HIV‐1 activity and cytotoxicity of 41 compounds is reported. Some structure‐activity relationships are discussed also in comparison with the known NPPS (2‐nitrop

ISSN:0365-6233    

DOI:10.1002/ardp.19953280304

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractEine Reihe von 3‐Mercaptoalkylthieno[2,3‐d]pyrimidin‐2,4(1H,3H)‐dionen3wurde synthetisiert und auf immunstimulatorische Wirksamkeit geprüft. Die Titelverbindungen wurden auf bequeme Weise durch hydrolytische Ringspaltung von thiazolo‐ bzw. 1,3‐thiazino‐anellierten Thienopyrimidinen1unter alkalischen oder auch sauren Bedingungen erhalten. Die ms Fragmentierung der Thieno[2,3‐d]pyrimidin‐2,4‐dione3wird diskutiert. Einige Verbindungen3zeigten in einer Hautreaktion vom verzögerten Typ (delayed type hypersensitivity; DTH) immunstimulatorische Aktivität im Wirkungsbe

ISSN:0365-6233    

DOI:10.1002/ardp.19953280305

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractAn efficient access to chiral, non racemic arylbutanols1a–c(ee>98%) as drug intermediates is described. Thioacetalization of substituted benzaldehydes3a–cwith 1,3‐propanedithiol gave 2‐aryl‐1,3‐dithianes4a–c. Lithiation of4a–cfollowed by reaction with racemic, (R)‐ or (S)‐propylene oxide, respectively, gave racemic, (R)‐ or (S)‐hydroxyalkyldithianes5a–cin high yields. Subsequent desulfurization with tributyltin hydride (TBTH) resulted in almost quantitative formation of the arylbutanols1a–c. Ketols6were obtained by hydrolysis of

ISSN:0365-6233    

DOI:10.1002/ardp.19953280306

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractSeveral (carbamoylalkenyl)‐ and (carbamoylalkenyl)phenyloxy carboxylic acids (Table 1) and some of their ethyl esters (Table 2) were synthesized and evaluatedin vitroas inhibitors of steroid 5α‐reductase. Inhibitors of this enzyme may be useful in treating dihydrotestosterone‐related diseases such as prostate cancer and benign prostatic hyperplasia. Using an enzyme preparation obtained from human prostate carcinoma tissue, the inhibition values ranged from 0 to 57 % at the given dose of 100 μM. In the series of free acids, surprisingly, the compounds showed only modest inhibitory potency (0–26 %). By contrast, the ethyl esters displayed inhibition values up to 57 %. Structure‐activity relationships ar

ISSN:0365-6233    

DOI:10.1002/ardp.19953280307

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractAusgehend vom käuflichen 6‐Methyl‐2‐pyridylamin (1) wurde über 12 Stufen das Pyrido[3,2‐e][1,4]diazepin14ain einer Gesamtausb. von 7% synthestisiert.14a, dasN‐Methyl‐Derivat14b, das Thiolactam15a, das Amidin16und das anellierte 1,2,4‐Triazol17wurden auf Anti‐HIV‐1‐Wirkung geprüft. Keine der geprüften Substanzen besitzt eine dem Zidovudin (3′‐Azido‐3′‐desoxythymidin = AZT) v

ISSN:0365-6233    

DOI:10.1002/ardp.19953280308

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractA new rapid and sensitive reversed‐phase HPLC method for the routine analysis of diclofenac in human plasma is described. The method shows high selectivity, sensitivity, and reproducibility employing 4′‐methoxydiclofenac as internal standard (IS) with UV‐detection at 282 nm. The correlation of peak area ratios (diclofenac/IS)versusdiclofenac plasma concentrations are linear between 5.0—2000 ng/ml with a detection limit of 3 ng/ml. Intra‐ and interday precision studies yielded coefficients of variation<6.2 % for all concentrations (range 20.0—1600 ng/ml). The method was applied for the assay of diclofenac in plasma of healthy volunteers after p.o. and rectal dosage of 50 mg diclofenac sodium and was found to be highly suitable for rou

ISSN:0365-6233    

DOI:10.1002/ardp.19953280309

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractDas 1,5‐Diketon3setzt sich mit Glycinestern bei Raumtemp. zu den Tetrahydrochinolinen5um. Bei niedrigerer Temp. bleibt die Reaktion auf der Stufe derN‐alkylierten 1,4‐Dihydropyridine (DHP)4stehen.4entsteht auch bei der Umsetzung von Glycinestern mit Acetylaceton und Formaldehyd in wäßrigem Pyridin. Weder4noch5sind mit dem photometrisch bestimmten Produkt der Farbreaktion nachPesez2,3)identisch. Mit den 1,5‐Dicarbonsäurediestern6werden die DH

ISSN:0365-6233    

DOI:10.1002/ardp.19953280310

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractStarting from natural asparagine (1) a synthesis of the protected (S)‐3,4‐diaminobutanenitriles5and8a–cviathe β‐homoserine derivative2is described. The amino function in position 4 was introduced byMitsunobu‐coupling or by reductive amination when a strange deformylation of the amino aldehyde7was observed as a side reaction. TheMitsunobu‐product5was converted into the dibenzylamine substituted GABA6bwhich was investigated for its affinity at the GAB

ISSN:0365-6233    

DOI:10.1002/ardp.19953280311

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY