Synthesis and anti-tubercular activity of a series of N’-substituted isonicotinohydrazide derivatives
Tuberculosis is a leading cause of death worldwide and especially in developing countries due to the recent emergence and spread of multi-drug resistant tuberculosis (MDR TB), extensive drug resistant tuberculosis (XDR TB), total drug resistant tuberculosis (TDR TB) and HIV/AIDS pandemic. Discovery of target based newer anti-tubercular agent is area of interest for chemists. We have designed a series of N’-substituted isonicotinohydrazide derivatives based on pharmacophore modeling. Designed molecules were synthesized and evaluated for their anti-tubercular activity. Among synthesized compounds, N’-(2-(2-fluorophenyl) acetyl) isonicotinohydrazide (4m) was found to be the most active compound with MIC value of 6.25 µg/ml against Mycobacterium tuberculosis H37Rv strain using Almar Blue method. Compound (4m) was found active against MDR-TB and XDR-TB strain at 62.5 and 250 µg/mL.
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