设计、合成、光谱分析和生物学评价可有效抑制细菌和真菌菌株的 1,3,4-噻二唑分子席夫碱

Sajid Ajit Malak, J. Rajput, Mustakim Sharif
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摘要

许多与众不同的天然和医药产品都包含众所周知的杂环核 1,3,4-噻二唑。本研究使用等摩尔量的 5-苯乙烯基-1,3,4-噻二唑-2-胺和取代的苯乙酮在乙醇的催化下合成了十种 1,3,4-噻二唑衍生物的希夫碱。合成的希夫碱衍生物通过傅立叶变换红外光谱、1H NMR、13C NMR 和质谱进行了表征。采用碟片扩散法测试了 1,3,4-噻二唑席夫碱(RM-1 至 RM-10)对铜绿假单胞菌、大肠杆菌、枯草芽孢杆菌、黑曲霉、烟曲霉和黄曲霉的体外抗菌活性。1,3,4-噻二唑席夫碱对细菌和真菌具有很强的抗菌活性,但其活性明显低于所评估的传统抗生素。
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Design, synthesis, spectral analysis, and biological evaluation of Schiff bases with a 1,3,4-thiadiazole moiety as an effective inhibitor against bacterial and fungal strains
Many distinct natural and pharmaceutical items include the well-known heterocyclic nucleus 1,3,4-thiadiazole. Ten Schiff bases of 1,3,4-thiadiazole derivatives have been synthesized using equimolar amounts of 5-styryl-1,3,4-thiadiazol-2-amine and substituted acetophenones in the catalytic amount of ethanol. The synthesized derivatives of Schiff's bases were characterized by FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. The 1,3,4-thiadiazole Schiff’s bases (RM-1 to RM-10) were tested for their in vitro antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis, Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus using the disc diffusion method. The 1,3,4-thiadiazole Schiff bases showed strong antibacterial activity against bacterial and fungal species, however, their activity was noticeably less effective than that of the evaluated conventional antibiotics.
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