Synthesis, antimicrobial activity, and biofilm inhibition studies of 1,2,3-triazole-containing 2,3-dihydrothiazole

IF 1.8 3区 化学 Q3 CHEMISTRY, ORGANIC
Ashraf A. Sediek , Asmaa F. Kassem , Mohamed S. Abdel-Aziz , Ahmed Younis
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引用次数: 0

Abstract

The newly synthesized 1,2,3-triazole-thiazole hybrids were first evaluated for their antimicrobial activity against different microbial strains. Most of it showed a marked selectivity against Gram-positive and Gram-negative bacterial strains. The MIC assay was then assessed; for S. aureus, 4a was equipotent to the reference neomycin, while 3a, 3b, and 8b were 2-fold lower. For E. coli, compounds 3a, 4a, and 8c were equipotent to neomycin, while 5a was 8-fold higher, and 8d was 2-fold higher. Most of tested compounds showed superiority to the reference drug against C. albicans; 8a and 8e showed MIC value of 16-fold higher than neomycin, while 3a was 8-fold higher. Also, 3b and 8f were 4-fold higher; 8d was 2-fold higher, while 5a was equipotent to neomycin against the same microbe. Further biofilm formation inhibition assay was conducted to the most active compounds, 5a was the most active against the three types of bacterial strains.

含 1,2,3-三唑的 2,3-二氢噻唑的合成、抗菌活性和生物膜抑制研究
首先对新合成的 1,2,3-三唑-噻唑混合物进行了抗菌活性评估,以检测它们对不同微生物菌株的抗菌活性。其中大部分对革兰氏阳性和革兰氏阴性细菌菌株具有明显的选择性。然后对 MIC 进行了评估;对于金黄色葡萄球菌,4a 与参照物新霉素相当,而 3a、3b 和 8b 则低 2 倍。对于大肠杆菌,化合物 3a、4a 和 8c 的耐药性与新霉素相当,而 5a 则高出 8 倍,8d 则高出 2 倍。大多数测试化合物对白茨球菌的作用优于参考药物;8a 和 8e 的 MIC 值比新霉素高出 16 倍,而 3a 则高出 8 倍。此外,3b 和 8f 的 MIC 值比新霉素高出 4 倍;8d 高出 2 倍,而 5a 对相同微生物的作用与新霉素相当。进一步对最有效的化合物进行了生物膜形成抑制试验,结果表明 5a 对三种细菌菌株最有效。
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来源期刊
Synthetic Communications
Synthetic Communications 化学-有机化学
CiteScore
4.40
自引率
4.80%
发文量
156
审稿时长
4.3 months
期刊介绍: Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.
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