Molecular modeling, synthesis, antibacterial and cytotoxicity evaluation of sulfonamide derivatives of benzimidazole, indazole, benzothiazole and thiazole

Bioorganic & Medicinal Chemistry
Farha NaazRamendra K Singh

Abstract

A new series of heterocyclic molecules bearing sulfonamide linkage has been synthesized and screened for antibacterial activity. During antibacterial screening using broath dilution method, molecules were found to be highly active (MIC value 50-3.1 µg/mL) against different human pathogens, namely B. cerus, S. aureus, E. coli and P. aeruginosa, and most effective against E. coli. A great synergistic effect was observed during determination of FIC where molecules were used in combination with reference drugs chloramphenicol and sulfamethoxazole. The MIC value of the combination - varying concentration of test compounds and ½ MIC of reference drugs or varying concentration of reference drugs and ½ MIC of test compounds, was reduced up to 1/4 or 1/32 of the original value, indicating thereby the combination was 4-32 times more potent than the test molecule. The molecules also showed low degree of cytotoxicity against PBM, CEM and VERO cell lines. The results positively indicated towards the development of lead antibacterials using the combination approach.

Citations

Jan 30, 2021·Bioorganic & Medicinal Chemistry Letters·Drashti G DarajiHitesh D Patel
Apr 9, 2021·Chemistry & Biodiversity·Helloana Azevedo-BarbosaDiogo Teixeira Carvalho
Jun 14, 2021·Bioorganic & Medicinal Chemistry Letters·Rammohan R Yadav BheemanaboinaCheng-He Zhou
Jul 14, 2021·Journal of Biomolecular Structure & Dynamics·Vishal K SinghRamendra K Singh
Aug 17, 2021·Bioorganic Chemistry·Himani ChaurasiaRamendra K Singh
Nov 27, 2020·Current Topics in Medicinal Chemistry·Congshan ShangGuoyan Cui
Jan 19, 2022·Drug Development Research·Cauê Benito Scarim, Fernando Rogério Pavan

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