Design, Synthesis, Characterization and Antitubercular Activity of Novel Benzimidazole Mannich Base Derivatives

Abstract

In present work, the newly synthesized benzimidazole Mannich base derivatives were design, synthesized and evaluated the in silico and in vitro antitubercular activity. These compounds were synthesized by condensation reaction between 1-(1H-benzo[d]imidazol-1-yl)ethanone and aliphatic/aromatic amines. The synthesized compound structures were identified by FTIR, 13C NMR, 1H NMR and mass spectroscopies. The results indicated that these derivatives have significant antitubercular activity against Mycobacterium tuberculosis (M.tb) cell wall enzyme enoyl acyl carrier protein reductase (InhA), EthR regulatory protein in H73Rv strain. The results found in the in vitro study are firmly similar to the in silico study. Among the synthesized compounds, 3d and 3e exhibited the highest activity due to the connection of the electron-donating group to the Mannich base. Therefore, these compounds deserve the development of new antitubercular agents.