Synthesis of novel substituted pyrazolyl-2-toluidinomethanethione and pyrazolyl-2-methoxyanilinomethanethione as potential antitubercular agents.
In the present investigation, a series of 5-[(substituted) phenyl]-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolyl-2-toluidinomethanethione and 5-[(substituted) phenyl]-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolyl-2-methoxyanilinomethanethione were synthesized and were tested for their antimycobacterial activity in vitro against isoniazid (INH) resistant Mycobacteium tuberculosis (INHR-MTB). Compound 6i was found to be the most potent derivative of the series with an MIC value of 0.90 mg/mL. When compared to INH, compound 6i was ca. 2-fold more active against INH resistant Mycobacterium tuberculosis (INHR-MTB).
Jamia Hamdard University, Department of Pharmaceutical Chemistry, Hamdard Nagar, New Delhi-110062, India.
Mohamed Ashraf
MA
Ali
Mohammad Shahar
MS
Yar
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests / Q000379:methods; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000235:genetics / Q000276:immunology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D011720:Pyrazoles