Synthesis and Anti-Tubercular Activity of Substituted Phenylpyrazole having Benzimidazole Ring Sabale Prafulla1,*, Bhagwat Dhiraj1, Sabale Vidya2 1Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, M.S 2Dadashab Balpande College of Pharmacy, Besa, Nagpur-440037, M.S. *Corresponding Author E-mail: prafullasable@yahoo.com
Online published on 31 October, 2018. Abstract Infectious microbial disease remains a major problem worldwide, because microbes have resisted prophylaxis or require longer therapy. Tuberculosis is most common and often deadly infectious disease caused by various strains of mycobacteria, usually Mycobacterium tuberculosis (M. Tb) in humans. Drugs used for tuberculosis are inadequate to address emerging challenge of treatment due to drug resistance towards the mycobacteria. A number of synthetic azole derivatives have been class of interest now days, which inhibits the synthesis of ergosterol in cell wall. They mainly inhibit 14α-demethylase enzyme, which is also present in the mycobacterium cell wall. The present study involves synthesis of substituted benzimidazole clubbed with pyrazole derivatives as 14α-demethylase inhibitor. The synthesized compounds were confirmed by analytical and spectroscopic techniques like m.p., TLC, IR, NMR and Mass spectroscopy. The compounds with high electronegative substituent show optimal activity against tuberculosis, while compound having less electronegative substituent showed less inhibitory activity. The compound having high molecular weight also showed good anti-tubercular activity. Among all synthesized compounds, 4B showed good anti-tubercular activity. Top Keywords Benzimidazole, Pyrazole, Anti-tubercular, Mycobacterium tuberculosis, 14α-Demethylase. Top |