Chloropyrimidines as a new class of antimicrobial agents
Chloropyrimidines as a new class of antimicrobial agents
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DOI：
10.1016/s0968-0896(01)00374-1
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发表时间：
2002-04-01
影响因子：
3.5
通讯作者：
Ram, VJ
中科院分区：
文献类型：
--
作者：
Agarwal, N;Srivastava, P;Ram, VJ
在我们研究嘧啶类化合物作为抗真菌药物的过程中，我们已经确定了一个亚类，在体外对分枝杆菌具有显著的活性。这些嘧啶类化合物(3a-o和7a，b)的显著特点是在第6位加了芳基、杂芳基和烷基硫基，在第2位加了烷基硫取代基。本文介绍了该化合物的合理设计、合成和体外抗结核分枝杆菌强毒株和非强毒株等6种病原菌的活性。部分化合物(3c、3h、3i、3o)在体外仅表现出较强的抗分枝杆菌活性，MIC值为0.75mug/m L，但3i在12.5m g/m L时也表现出对大肠杆菌的抑制活性。只有化合物3a和3b对铜绿假单胞菌和大肠埃希菌有抗菌活性，其MIC值分别为12.5µg/mL。所有合成的化合物对5种病原真菌也有抑菌活性，但只有部分化合物3j-n和7a，b对烟曲霉和须毛霉菌有最强的抑菌活性。(C)2002爱思唯尔科学有限公司。保留所有权利。
In the course of our investigations of pyrimidines as antimycotic agents, we have identified a sub-class, with significant in vitro activity against mycobacteria. The salient feature of these pyrimidine derivatives (3a-o and 7a,b) is their appended aryl, heteroaryl and alkylthio substituent at position 6 and also alkylthio substituent at position 2. The rational design, synthesis, and evaluation of the in vitro antibacterial activity against six pathogenic bacteria including virulent and non-virulent strains of Mycobacterium tuberculosis is described. Some of the synthesized compounds (3c, 3h, 3i, 3o) have displayed only potent in vitro antimycobacterial activity with MIC of 0.75 mug/mL except 3i which also demonstrated activity against Escherichia coli at 12.5 mug/ mL concentration. Only two compounds, 3a and 3b, demonstrated antibacterial activity against Pseudomonas aeruginosa and E. coli with MIC 12.5 mug/mL. All the synthesized compounds were also evaluated for their antimycotic activity against five pathogenic fungi but only some of them 3j-n and 7a,b were found most potent against Aspergillus fumigatus and Trichophyton mentagrophytes. (C) 2002 Elsevier Science Ltd. All rights reserved.