New thiazolo[4,5-d]pyrimidine derivatives as potential antimicrobial agents

被引：0
作者：
Urgun, H
Balkan, A [1 ]
Özalp, M
机构：
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, Ankara, Turkey
[2] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Microbiol, Ankara, Turkey
来源：
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH | 2000年 / 50卷 / 12期
关键词：
2-thioxothiazolo[4,5-d]pyrimidin-7(6H)-ones; antibacterial activity; antifungal activity; in vitro studies; synthesis;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In this study, by starting from ethyl 4-amino-2,3-dihydro-3-phenyl-2-thioxothiazole-5-carboxylate (1), three compounds having 2,3-dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thioxothiazolo [4,5-d]pyrimidin-7(6H)-one (2a-c) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-1) were synthesized. The antimicrobial activities of the synthesized compounds were investigated against some bacteria and fungi using the microdilution method. 2.3-Dihydro-3,6-diphenyl-5-(4'-bromobenzoylmethyl)thio-2-thioxothiazolo[4,5-d]pyrimidin-7(6H) one (3k) possessing remarkable activity against Gram-positive bacteria and yeast like fungi was found to be the most active compound in this series.
引用
收藏
页码：1115 / 1119
页数：5
相关论文
共 17 条
[1]   POTENTIAL ANTI-MICROBIALS .1. SYNTHESIS AND STRUCTURE-ACTIVITY STUDIES OF SOME NEW THIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES [J].
BADAWEY, ESAM ;
RIDA, SM ;
HAZZA, AA ;
FAHMY, HTY ;
GOHAR, YM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (02) :91-96
[2]   POTENTIAL ANTI-MICROBIALS .2. SYNTHESIS AND INVITRO ANTIMICROBIAL EVALUATION OF SOME THIAZOLO[4,5-D]PYRIMIDINES [J].
BADAWEY, ESAM ;
RIDA, SM ;
HAZZA, AA ;
FAHMY, HTY ;
GOHAR, YM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (02) :97-101
[3]   THIAZOLO[5,4-D]PYRIMIDINE DERIVATIVES AS AMPLIFIERS OF PHLEOMYCIN AGAINST ESCHERICHIA-COLI [J].
BROWN, DJ ;
DUNLAP, WC ;
GRIGG, GW ;
KELLY, J .
AUSTRALIAN JOURNAL OF CHEMISTRY, 1977, 30 (08) :1775-1783
[4]  
DEVANI MB, 1977, ARZNEIMITTELFORSCH, V27, P1652
[5]   HETEROCYCLEN AUS CH-ACIDEN NITRILEN .6. REAKTION VON METHYLENAKTIVEN NITRILEN MIT SENFOLEN UND SCHWEFEL [J].
GEWALD, K .
JOURNAL FUR PRAKTISCHE CHEMIE, 1966, 32 (1-2) :26-&
[6]  
Habib NS, 1996, MONATSH CHEM, V127, P1203, DOI 10.1007/BF00844696
[7]   Condensed thiazoles .2. Synthesis of 7-substituted thiazolo[4,5-d]pyrimidines as possible anti-HIV, anticancer, and antimicrobial agents [J].
Habib, NS ;
Rida, SM ;
Badawey, EAM ;
Fahmy, HTY .
MONATSHEFTE FUR CHEMIE, 1996, 127 (11) :1209-1214
[8]   beta-naphthyl derivatives of ethanolamine and n-substituted ethanolamines [J].
Immediata, T ;
Day, AR .
JOURNAL OF ORGANIC CHEMISTRY, 1940, 5 (05) :512-527
[9]  
KENITH RR, 1987, Patent No. 136020
[10]   SYNTHESIS AND ANTIVIRAL ACTIVITY OF CERTAIN GUANOSINE ANALOGS IN THE THIAZOLO[4,5-D]PYRIMIDINE RING-SYSTEM [J].
KINI, GD ;
ANDERSON, JD ;
SANGHVI, YS ;
LEWIS, AF ;
SMEE, DF ;
REVANKAR, GR ;
ROBINS, RK ;
COTTAM, HB .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (10) :3006-3010
12