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A series of new benzimidazole incorporated 3,5-bis (arylidene)-4-piperidones were synthesized by using aryl aldehydes, piperidinone, 2-(chloromethyl)-benzimidazole and DBU acetate [DBUH][OAc] act as a catalyst under solvent free condition in excellent yields. The synthesized compounds were screened for their  in vitro  antimycobacterial activity against  M. tuberculosis  H37Ra ( MTB ) and  M. bovis  BCG strains. The compounds  4a ,  4b ,  4e ,  4i ,  4k  and  4l  are highly potent against both the strains. Most of the active compounds are non-cytotoxic against MCF-7, A549, HCT 116 and THP-1 cell lines. Furthermore, a molecular docking study of these compounds was carried out to investigate their binding pattern with the target, active site of mycobacterial enoyl-acyl carrier protein reductase (Inh A). Therefore, these compounds can be subjected for further optimization and drug development which could give promising chemical leads for treatment of TB.

[DBUH][OAc]-Catalyzed Domino Synthesis of Novel Benzimidazole Incorporated 3,5-Bis (Arylidene)-4-Piperidones as Potential Antitubercular Agents