摘要:

AbstractThe study concerns new syntheses of 5‐hydroxy ether and 5‐aminohydroxy ether derivatives of pyrimidine. When tested for antibacterial activity, some of the compounds exhibited promising effe

ISSN:0365-6233    

DOI:10.1002/ardp.19973300802

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractIndolones of the general formula1(Fig. 1 and 2) can act as Michael substrates, which readily add various nucleophiles. 1,4‐Addition of S‐nucleophiles to these indolones gives access to compounds of the general formula2(Fig. 2). The addition is reversible, meaning that these compounds behave as prodrugs of the (in‐vitro) cyto‐toxic indolones. The addition products possess less cytotoxicity of their own, but can presumably release the parent indolones in‐vivo. This behaviour makes them valuable compounds, allowing their use as cytotoxic agents. Furthermore, some of the addition products possess antibiotic activity, making them worth testing as agents against certain microbes. Their specificity towards certain microorganisms, which does not fit the usual scheme of activity towards gram positive or gram negative bacteria, is remarkable and needs further ver

ISSN:0365-6233    

DOI:10.1002/ardp.19973300803

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractBoth 2‐nitrooxymethyl‐4‐phenyl‐ (2) and 4‐nitrooxymethylphenyl‐1,4‐dihydropyridines (3) represent new combinations of two different vasodilating structures.2could not be isolated due to its spontaneous lactonization. Derivatives of3were obtainedviaHantzsch synthesis using nitrooxymethylated benzaldehydes. The inotropic potency in isolated porcine trabecular muscles and the vasodilator activity in isolated porcine coronary arteries of four nitrooxyphenyl‐dihydropyridines were determined. Nitrendipine (NTD) and glyceryl trinitrate (GTN) were used for reference.3were negative inotropic, however, less than NTD and ‐ except for the dicyano derivative3d‐ more than GTN. Vasodilator properties were less pronounced than that of both nitrendipine and GTN. Vascular

ISSN:0365-6233    

DOI:10.1002/ardp.19973300804

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

Abstract1‐Benzylbenzimidazole reacts with chloromethylalkyl ethers or sulfides or chloromethylcycloalkyl ethers to produce 3‐alkoxy‐methyl‐1‐benzylbenzimidazolium or 3‐alkylthiomethyl‐1‐benzylbenzimidazolium or 1‐benzyl‐3‐cycloalkoxymethylbenzimidazolium chlorides in very good yields. All the 1‐benzylbenzimidazolium chlorides showed antimicrobial activity. The relationship between chemical structure and antimicrobial activity was analyzed by quantitative structure‐acti

ISSN:0365-6233    

DOI:10.1002/ardp.19973300805

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractA group of 5‐ethyl‐5‐halo‐6‐alkoxy (or azido)‐5,6‐dihydro‐2′‐deoxyuridines, which differ in configuration at the C‐5 and C‐6 positions, were synthesized by the regiospecific addition of XR (X = I, Br, Cl; R = alkoxyl, azido) to the 5,6‐olefinic bond of 5‐ethyl‐2′‐deoxyuridine (EDU).In vitroantiviral (HSV‐1, HSV‐2, HCMV, VZV) activities were determined. Structure‐activity studies showed that the C‐5 halogeno (I, Br, Cl) and C‐6 alkoxy (OMe, OEt) or azido, substituents were determinants of antiviral activity where the (5R,6R)‐5and (5S,6S)‐6diastereomers of 5‐ethyl‐5‐iodo‐6‐methoxy‐5,6‐dihydro‐2′‐deoxyuridine exhibited greater potency against HSV‐1, HSV‐2, and HCMV than the related 5‐chloro‐6‐ethoxy and 5‐bromo (or chloro)‐6‐azido diastereomers. The most potent antiviral agents, (+)‐trans‐(5R,6R)‐5and (−)‐trans‐(5S,6S)‐6diastereomers of 5‐ethyl‐5‐iodo‐6‐methoxy‐5,6‐dihydro

ISSN:0365-6233    

DOI:10.1002/ardp.19973300806

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

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 tumo

ISSN:0365-6233    

DOI:10.1002/ardp.19973300807

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe synthesis of a new series of 1β‐methylcarbapenems having a 1,3‐diazabicyclo[3.3.0]octane‐2,4‐dione moiety is described. Theirin vitroantibacterial activities against both Gram‐positive and Gram‐negative bateria are determined and the effect of substituent on the bicyclic ring as well as stereoisomerism was

ISSN:0365-6233    

DOI:10.1002/ardp.19973300808

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19973300801

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY