Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125001, India
Med Chem. 2013 Feb;9(1):53-76. doi: 10.2174/157340613804488404.
A series of N(2)-acyl isonicotinic acid hydrazides (1-17) was synthesized and tested for its in vitro antimycobacterial activity against Mycobacterium tuberculosis and the results indicated that the compound, isonicotinic acid N'- tetradecanoyl-hydrazide (12) was more active than the reference compound isoniazid. The results of antimicrobial activity of the synthesized compounds against S. aureus, B. subtilis, E. coli, C. albicans and A. niger indicated that compounds with dichloro, hydroxyl, tri-iodo and N(2)-tetradecanoyl substituent were the most active ones. The antiviral activity studies depicted that none of the tested compounds were active against DNA or RNA viruses. The multi-target QSAR model was found to be effective in describing the antimicrobial activity of N(2)-acyl isonicotinic acid hydrazides.
合成了一系列 N(2)-酰基异烟酰肼（1-17），并对其进行了体外抗结核分枝杆菌活性测试，结果表明，化合物异烟酰肼 N'-十四酰基酰肼（12）比对照化合物异烟肼更具活性。合成化合物对金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌、白色念珠菌和黑曲霉的抗菌活性结果表明，具有二氯、羟基、三碘和 N(2)-十四酰基取代基的化合物具有最强的活性。抗病毒活性研究表明，没有一种测试化合物对 DNA 或 RNA 病毒具有活性。多靶点 QSAR 模型被发现能够有效地描述 N(2)-酰基异烟酰肼的抗菌活性。
