首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and in vitro antimicrobial activity of novel N -(6-chlorobenzo[ d ]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class
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Synthesis and in vitro antimicrobial activity of novel N -(6-chlorobenzo[ d ]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class

机译:新型苯并噻唑类N-(6-氯苯并[d]噻唑-2-基)肼甲酰胺衍生物的合成及体外抗菌活性

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In this study, a series of novel 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a–g) and 1,3,4-oxadiazole (7a–g, 8) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (?) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5–100?μg/mL in DMSO. It has been observed that triazolo-thiadiazole derivatives are found to be more active than 1,3,4-oxadiazole derivatives against all pathogenic bacterial and fungal strains.
机译:在这项研究中,一系列新颖的1,2,4-三唑-[3,4-b] -1,3,4-噻二唑(6a–g)和1,3,4-恶二唑(7a–g,8 )由苯并噻唑类的N-(6-氯苯并[d]噻唑-2-基)肼甲酰胺衍生物合成。研究了标题化合物衍生物对一种革兰氏+细菌(金黄色葡萄球菌),三种革兰氏(α)细菌(大肠杆菌,铜绿假单胞菌,肺炎克雷伯菌)和五种真菌(白色念珠菌,黑曲霉,黄曲霉,使用连续平板稀释法提取紫癜和柠檬青霉。抗菌和抗真菌筛选数据的调查显示,所有测试的化合物在DMSO中的12.5–100?μg/ mL均显示出中度到良好的抑制作用。已经发现,对所有病原性细菌和真菌菌株,三唑并噻二唑衍生物比1,3,4-恶二唑衍生物更具活性。

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