含 2,4-二取代噻唑环的新型席夫碱的合成、抑菌和抗真菌活性。
Synthesis, anti-bacterial and anti-fungal activities of some novel Schiff bases containing 2,4-disubstituted thiazole ring.
机构信息
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi 221005, India.
出版信息
Eur J Med Chem. 2010 Feb;45(2):651-60. doi: 10.1016/j.ejmech.2009.11.008. Epub 2009 Nov 6.
A series of arylidene-2-(4-(4-methoxy/bromophenyl) thiazol-2-yl) hydrazines (4a-z) and 1-(4-(4-methoxy/bromophenyl) thiazol-2-yl)-2-cyclohexylidene/cyclopentylidene hydrazines (5a-b/6a-b) were synthesized, characterized and screened for their antimicrobial activities. The structures of synthesized compounds were established by spectroscopic (FT-IR, (1)H NMR, (13)C NMR, Mass) and elemental analyses. Both the anti-bacterial and anti-fungal activities with MIC values of compounds were evaluated. The results of anti-bacterial screening reveal that among all the compounds screened eight compounds showed moderate to good anti-bacterial activity while ten of the newly synthesized compounds displayed good to excellent anti-fungal activity. Among the tested compounds, the most effective compounds with MIC value in the range of 6.25-25 microg/ml are 4a, 4n, 4z, 5a, 5b, 6a and 6b against three fungal strains viz. Candida albicans, Cryptococcus neoformans and Aspergillus flavus.
一系列芳基-2-(4-(4-甲氧基/溴苯基)噻唑-2-基)腙(4a-z)和 1-(4-(4-甲氧基/溴苯基)噻唑-2-基)-2-环己基/环戊基腙(5a-b/6a-b)被合成、表征，并对其抗菌活性进行了筛选。合成化合物的结构通过光谱(FT-IR、(1)H NMR、(13)C NMR、质量)和元素分析来确定。用 MIC 值评估了化合物的抗细菌和抗真菌活性。抗细菌筛选的结果表明，在所筛选的化合物中，有 8 种化合物表现出中等至良好的抗细菌活性，而新合成的 10 种化合物表现出良好至优异的抗真菌活性。在所测试的化合物中，具有 MIC 值在 6.25-25 μg/ml 范围内的最有效化合物是 4a、4n、4z、5a、5b、6a 和 6b，它们对三种真菌菌株，即白色念珠菌、新生隐球菌和黄曲霉，具有活性。
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