噻唑并[4,5-d]嘧啶衍生物作为潜在抗菌剂的合成。

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

作者信息

Habib Nargues S, Soliman Raafat, El-Tombary Alaa A, El-Hawash Soad A, Shaaban Omaima G

机构信息

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

出版信息

Arch Pharm Res. 2007 Dec;30(12):1511-20. doi: 10.1007/BF02977319.

DOI:10.1007/BF02977319

PMID:18254237

Abstract

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]-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coil and P. aeruginosa, and all were inactive against S. aureus.

摘要

在本研究中，我们报告了几种新型噻唑并[4,5-d]嘧啶衍生物的合成及抗菌活性评估，即7-取代氨基-5-甲基-3-苯基噻唑并[4,5-d]嘧啶-2(3H)-硫酮4a-e、8、13、15，2-氰基-2-(7-取代-5-甲基-3-苯基噻唑并[4,5-d]嘧啶-2(3H)-亚基)乙酸乙酯5a-b，2-(7-取代-5-甲基-3-苯基噻唑并[4,5-d]嘧啶-2(3H)-亚基)丙二腈6a-b，5-甲基-7-吗啉代-3-苯基噻唑并[4,5-d]嘧啶-2(3H)-酮7，以及7-[4-(1-取代-5-苯基-4,5-二氢-1H-吡唑啉-3-基)苯胺基]-5-甲基-3-苯基噻唑并[4,5-d]嘧啶-2(3H)-硫酮10-12。一些受试化合物对白色念珠菌的活性比对大肠杆菌和铜绿假单胞菌更强，且所有化合物对金黄色葡萄球菌均无活性。