期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 15, 页码 3947-3949出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.05.024
关键词
antimycobacterial activity; pyrazolines
A series of N-1-nicotinoyl-3- (4'-hydroxy-3'-methyl phenyl)-5-(substituted phenyl)-2-pyrazolines were synthesized by the reaction between isoniazid (INH) and chalcones and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) using the agar dilution method. Among the synthesized compounds, compound (i) N-1-nicotinyl-3-(4'-hydroxy-3'-methyI phenyl)-5-(1-chlorophenyl)-2-pyrazoline was found to be the most active agent against MTB and INHR-MTB, with minimum inhibitory concentration of 0.26 mu m. When compared to INH-compound i was found to be 2.8- and 43.7-fold more active against MTB and INHR-MTB, respectively. (c) 2006 Elsevier Ltd. All rights reserved.
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