Docking Stimulations and Primary Assessment of Newly Synthesized Benzene Sulfonamide Pyrazole Oxadiazole Derivatives as Potential Antimicrobial and Antitubercular Agents

A novel series of benzene sulfonamide pyrazole oxadiazole derivatives have been synthesized by reaction of 4-(5-(3-fluoro-4-methoxyphenyl)-3-(hydrazinecarbonyl)-1H-pyrazol-1-yl) benzene sulfonamide with different substituted benzoic/pyridinyl/indolyl acids in phosphorous oxychloride, characterized by IR, H-1 NMR, C-13 NMR, MS analytical data and evaluated for their antimicrobial as well as antitubercular activity. Molecular docking studies against Mycobacterium tuberculosis beta-ketoacyl-acyl carrier protein synthase A, (Kas-A) was carried out to understand the possible mode of its inhibition and potential of synthesized compounds as antitubercular agents. Antibacterial activity of compounds 5d (3-Cl) and 5f (2,4-diCl) were found good against E. coli, P. aeruginosa, S. aureus and S. pyogenes as compared to standard Ampicillin. Compound 5d was found active antitubercular agents against M. tuberculosis H(37)Rv.

Automated summary

A series of novel benzene sulfonamide pyrazole oxadiazole derivatives were synthesized and evaluated for their antimicrobial and antitubercular activity. Compound 5d showed good antibacterial activity against several bacterial strains and also exhibited antitubercular activity against Mycobacterium tuberculosis.