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新型硫代缩氨基脲衍生物的合成、抗菌和抗癌活性。

Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives.

机构信息

Medicinal Chemistry Research Division, Vaagdevi College of Pharmacy, Hanamkonda, Andhra Pradesh, India.

出版信息

Arch Pharm (Weinheim). 2011 Feb;344(2):84-90. doi: 10.1002/ardp.201000201. Epub 2010 Nov 25.

Abstract

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC(50) value of about 1 µM. Compound 4f showed potent antifungal activity against Candida albicans (IC(50)  = 1.29 µM) and compound 4h showed potent anticancer activity (IC(50)  = 0.07 µM).

摘要

对对氨基苯甲酸的缩氨硫脲进行了合成,并测试了它们的抗菌和抗癌活性。发现羟肟酸衍生物 4a-4l 比其相应的酸具有更好的抗菌和抗癌活性。化合物 4d 对大肠杆菌、肺炎克雷伯菌、金黄色葡萄球菌、霍乱弧菌和枯草芽孢杆菌具有良好的抗菌活性,IC(50) 值约为 1µM。化合物 4f 对白色念珠菌表现出很强的抗真菌活性(IC(50) = 1.29µM),化合物 4h 表现出很强的抗癌活性(IC(50) = 0.07µM)。

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