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

被引:32
作者
Habib, Nargues S. [1 ]
Solliman, Raafat [1 ]
El-Tombary, Alaa A. [1 ]
El-Hawash, Soad A. [1 ]
Shaaban, Omaima G. [1 ]
机构
[1] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21251, Egypt
关键词
thiazolo[4,5-d]pyrimidines; pyrazolines; antimicrobial;
D O I
10.1007/BF02977319
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5-d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7-substituted-5-methyl-3-phenylthiazolo[4,5-d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d] pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E coli and P aeruginosa, and all were inactive against S. aureus.
引用
收藏
页码:1511 / 1520
页数:10
相关论文
共 20 条
[1]   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
[2]   Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists [J].
Beck, JP ;
Curry, MA ;
Chorvat, RJ ;
Fitzgerald, LW ;
Gilligan, PJ ;
Zaczek, R ;
Trainor, GL .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (08) :1185-1188
[3]  
BECK JP, 1999, BIOORG MED CHEM LETT, V131, pE8797
[4]   Design and synthesis of some substituted 1H-pyrazolyl-thiazolo[4,5-d]pyrimidines as anti-inflammatory-antimicrobial agents [J].
Bekhit, AA ;
Fahmy, HTY ;
Rostom, SAF ;
Baraka, AM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2003, 38 (01) :27-36
[5]  
BEKHIT AA, 2003, EUR J MED CHEM, V139, pH5292
[6]  
EATEDAL HA, 2002, MONATSH CHEM, V133, P255
[7]  
Fahmy H. T. Y, 2003, ARCH PHARM PHARM MED, V3, P1
[8]  
Farghaly A M, 2002, Boll Chim Farm, V141, P372
[9]  
Farghaly AA, 2000, ARCH PHARM, V333, P53, DOI 10.1002/(SICI)1521-4184(200002)333:2/3<53::AID-ARDP53>3.0.CO
[10]  
2-E