Synthesis and antitubercular activity of substituted novel pyrazoline derivatives.
A series of 2-2-methoxy-4-[5-(substituted phenyl)1-(4-pyridylcarbonyl)-4,5-dihydro-1H-3-pyrazolyl] phenoxyacetic acid were synthesized by the reaction between isoniazid (INH) and chalcones, and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv and INH resistant M. tuberculosis using BACTEC-460 radiometric system and agar dilution method. Among the synthesized compounds, Compounds II 2-4-[5-(4-hydroxyphenyl)-1-(4-pyridylcarbonyl)-4,5-ihydro-1H-3-pyrazolyl]-2-methoxy phenoxy acetic acid was found to be most active agent against M. tuberculosis H37Rv (MTB) and INH resistant M. tuberculosis (INHR-MTB), with minimum inhibitory concentration of 0.12 microM, when compared to INH 5.6-fold more active against MTB and 78-fold more active against INHR-MTB, respectively.
Ali
Mohamed Ashraf
MA
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard University, New Delhi-110062, India. asraf80med@rediffmail.com
Yar
Mohammad Shahar
MS
Kumar
Mahesh
M
Pandian
Ganesan Suresh
GS
D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047188:Chalcones / Q000737:chemistry; D007538:Isoniazid / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D000085:Acetates; D000995:Antitubercular Agents; D047188:Chalcones; D011720:Pyrazoles; D007538:Isoniazid