A new series of 1-(4-methyl-2-aryl-1,3-thiazol-5-yl)-2-(4-aryl-1,2,3-triazol-1-yl)ethanol (6a-t) have been synthesized by a click reaction of 2-azido-1-(4-methyl-2-phenylthiazol-5-yl)ethanone (3a-e) with substituted ethynylbenzene (4a-c) followed by reduction with sodiumboro hydride. The newly synthesized 1-(4-methyl-2-aryl-1,3-thiazol-5-yl)-2-(4-aryl-1,2,3-triazol-1-yl)ethanol derivatives were screened for in vitro antibacterial activityagainst a Gram negative strains, Escherichia coli (National Collection of Industrial Microorganisms, NCIM 2574), a Gram positive strain Staphylococcus albus (NCIM 2178) and in vitro antifungal activity against Candida albicans (NCIM 3100), Aspergillus niger (American Type Culture Collection, ATCC 504), Rhodotorula glutinis (NCIM 3168), and Penicillium chrysogenum (NCIM 737). Eight thiazolyl-1,2,3-triazolyl-alcohol derivatives 6a, 6i, 6j, 6k, 6m, 6n, 6o, and 6p, reported promissing antifungal activity against A. niger with minimum inhibitory concentration (MIC) 31.25–62.5 µg/mL. Compounds 6d, 6m, and 6p showed good antibacterial activity against S. albus. It was revealed that, 4-chlorophenyl and 4-fluorophenyl group at position-2 of thiazole ring reported good activity against A. niger. The substantial antimicrobial activity of 1-(4-methyl-2-aryl-1,3-thiazol-5-yl)-2-(4-aryl-1,2,3-triazol-1-yl)ethanol derivatives suggested that, these compounds could assist in the development of lead compounds as a treatment against microbial infection.

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新型噻唑基1,2,3-三唑基醇衍生物的合成及抗菌性能评价

1-（4-甲基-2-芳基-1,3-噻唑-5-基）-2-（4-芳基1,2,3-三唑-1-基）乙醇（6a-t）的新系列）是通过2-叠氮基-1-（4-甲基-2-苯基噻唑-5-基）乙酮（3a-e）与取代的乙炔基苯（4a-c）的点击反应合成，然后用硼氢化钠还原而合成的。筛选了新合成的1-（4-甲基-2-芳基-1,3-噻唑-5-基）-2-（4-芳基1,2,3-三唑-1-基）乙醇衍生物。革兰氏阴性菌株，大肠杆菌（国家工业微生物保藏中心，NCIM 2574），革兰氏阳性菌株白葡萄球菌（NCIM 2178）的体外抗菌活性以及对白色念珠菌（NCIM 3100），黑曲霉的体外抗真菌活性（美国典型培养物保藏中心，ATCC 504），Rhodotorula glutinis（NCIM 3168）和Chensogenum chrysogenum（NCIM 737）。八种噻唑基-1,2,3-三唑基-醇衍生物6a，6i，6j，6k，6m，6n，6o和6p，据报道对黑曲霉具有抗真菌活性，最低抑菌浓度（MIC）为31.25–62.5 µg /毫升 6d的化合物，6M和6P显示对良好的抗菌活性S.黄鳝。结果表明，噻唑环第2位的4-氯苯基和4-氟苯基具有良好的抗黑曲霉活性。。1-（4-甲基-2-芳基-1,3-噻唑-5-基）-2-（4-芳基-1,2,3-三唑-1-基）乙醇衍生物的基本抗菌活性表明，这些化合物可协助开发先导化合物来抵抗微生物感染。