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一些作为抗菌剂的2,5-二取代苯并恶唑和苯并咪唑的合成及其构效关系

Synthesis and structure-activity relationships of some 2,5-disubstituted benzoxazoles and benzimidazoles as antimicrobial agents.

作者信息

Sener E, Yalçin I, Temiz O, Oren I, Akin A, Uçartürk N

机构信息

Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Turkey.

出版信息

Farmaco. 1997 Feb;52(2):99-103.

PMID:9181690
Abstract

The synthesis of a new series of 2,5-disubstitutedbenzoxazoles 5a-e, and 2,5-disubstitutedbenzimidazoles 6a-h are described in order to determine their antimicrobial activities and feasible structure-activity relationships (SAR). The synthesized compounds were tested in vitro against 3 Gram-positive, 3 Gram-negative, bacteria and a fungus Candida albicans. 5c, and 5e were found most active than the others against Bacillus subtilis at a MIC value of 3.12 micrograms/ml and the compounds 5e, 6a and 6e indicated significant antibacterial activity against the enterobacter Pseudomonas aeruginosae. 5a, 5c, 5d and 6d also exhibited antimycotic activity against C. albicans. The antibacterial and antimycotic activities of 5-6 are compared with several control drugs.

摘要

为了确定一系列新的2,5 - 二取代苯并恶唑5a - e和2,5 - 二取代苯并咪唑6a - h的抗菌活性以及可行的构效关系(SAR),本文描述了它们的合成过程。合成的化合物针对3种革兰氏阳性菌、3种革兰氏阴性菌以及白色念珠菌进行了体外测试。发现5c和5e对枯草芽孢杆菌的活性最高,其最低抑菌浓度(MIC)值为3.12微克/毫升,并且化合物5e、6a和6e对铜绿假单胞菌显示出显著的抗菌活性。5a、5c、5d和6d对白色念珠菌也表现出抗真菌活性。将5 - 6的抗菌和抗真菌活性与几种对照药物进行了比较。

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