Synthesis and in vitro antimycobacterial activity of N-nicotinoyl-3-(4'- hydroxy-3'-methyl phenyl)-5-[(sub)phenyl]-2-pyrazolines

A series of N-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-resista...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-08, Vol.16 (15), p.3947-3949
Hauptverfasser: Shaharyar, Mohammad, Siddiqui, Anees Ahamed, Ali, Mohamed Ashraf, Sriram, Dharmarajan, Yogeeswari, Perumal
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Sprache:eng
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Zusammenfassung:A series of N-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-nicotinyl-3-(4'-hydroxy-3'-methyl 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.05.024