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含吲哚的1,3,4-噻二唑、1,2,4-三唑衍生物及其开链类似物的合成与抗菌活性评价

Synthesis and antimicrobial evaluation of indole containing derivatives of 1,3,4-thiadiazole, 1,2,4-triazole and their open-chain counterparts.

作者信息

Tsotinis A, Varvaresou A, Calogeropoulou T, Siatra-Papastaikoudi T, Tiligada A

机构信息

Department of Pharmacy, University of Athens, Greece.

出版信息

Arzneimittelforschung. 1997 Mar;47(3):307-10.

PMID:9105551
Abstract

The increasing clinical importance of drug-resistant bacterial pathogens has lent additional urgency to microbiological and antibacterial research. New indolic derivatives of triazoles, thiadiazoles and their respective open-chain thiosemicarbazides were evaluated for antibacterial and antifungal activity. The microorganisms used were the Gram-negative bacteria Escherichia coli ATCC 35218 and Pseudomonas aeruginosa ATCC 27853, the Gram-positive bacteria Staphylococcus aureus ATCC 25923 and Bacillus subtilis BBL 12084 and the yeasts Candida and Saccharomyces cerevisiae ATCC 2366. The most potent compounds were indole derivatives (12a-c) bearing 1,2,4-triazo-thien-5-yl moiety, which exhibit interesting antibacterial and antifungal activities.

摘要

耐药性细菌病原体在临床上的重要性日益增加,这使得微生物学和抗菌研究变得更加紧迫。对三唑、噻二唑及其各自的开链硫代氨基脲的新型吲哚衍生物进行了抗菌和抗真菌活性评估。所使用的微生物包括革兰氏阴性菌大肠杆菌ATCC 35218和铜绿假单胞菌ATCC 27853、革兰氏阳性菌金黄色葡萄球菌ATCC 25923和枯草芽孢杆菌BBL 12084以及酵母念珠菌和酿酒酵母ATCC 2366。最有效的化合物是带有1,2,4-三唑-噻吩-5-基部分的吲哚衍生物(12a - c),它们表现出有趣的抗菌和抗真菌活性。

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