Synthesis and Evaluation of New Thiazole Derivatives as Potential Antimicrobial Agents

被引：6

作者：

Altintop, Mehlika Dilek ^{[1
]}

Ozdemir, Ahmet ^{[1
]}

Atli, Ozlem ^{[1
]}

Canturk, Zerrin ^{[2
]}

Baysal, Merve ^{[1
]}

Kaplancikli, Zafer Asim ^{[1
]}

机构：

[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey

[2] Anadolu Univ, Fac Pharm, Dept Pharmaceut Microbiol, Eskisehir, Turkey

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2016年 / 13卷 / 09期

关键词：

Thiazole; hydrazone; piperidine; antimicrobial activity; cytotoxicity; genotoxicity; IN-VITRO EVALUATION; BIOLOGICAL EVALUATION; HYDRAZONE DERIVATIVES; ANTITUBERCULOSIS ACTIVITY; ANTIBACTERIAL; IDENTIFICATION; RESISTANCE; DESIGN;

D O I：

10.2174/1570180813666160226001021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an effort to develop potent antimicrobial agents, new thiazolyl hydrazone derivatives were synthesized and investigated for their inhibitory effects on pathogenic bacteria and yeasts. MTT assay was carried out to determine the cytotoxic effects of the compounds on NIH/3T3 mouse embryonic fibroblast cell line. Among these compounds, 2-[2-[1-(4-(piperidin-1-yl)phenyl)ethylidene] hydrazinyl]-4-(4-fluorophenyl) thiazole (7) exhibited notable antimicrobial activity against Enterococcus faecalis (ATCC 51922), Pseudomonas aeruginosa, Escherichia coli (ATCC 35218), Candida krusei, Candida glabrata and Candida parapsilosis. Due to its promising antimicrobial activity, the mutagenic potential of compound 7 was also evaluated by means of Ames test. According to MTT and AMES assays, this compound was identified as non-toxic and non-mutagenic.

引用

页码：903 / 911

页数：9

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