Benzimidazole-core as an antimycobacterial agent

- Benzimidazole core is an attractive target for drug development.
- In this review we discussed benzimidazole as antitubercular agent.
- Review analyzes structural requirements of benzimidazole as anti-TB agents, with SAR study.
- Review will be helpful for new thoughts in the quest for rational designs anti-TB drugs.

Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India's most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce significant antiTB potential. To seek more insights on this unique feature of benzimidazole candidates, there is an urgency to assemble the recent advances in this promising area. This review presents an overview of the recent advancements and focuses on the structural features responsible for unique antiTB applications and compiled published reports on benzimidazole derivatives emphasizing on different approaches employed for their syntheses in order to help medicinal and clinical chemists in designing next generation, yet effective and safer antiTB candidates.

Within the vast range of heterocycles, benzimidazole and its derivatives are found to be trendy structures employed for discovery of drugs in the field of pharmaceutical and medicinal chemistry. The unique structural features of benzimidazole and a wide range of biological activities of its derivatives made it privileged structure in drug discovery. The related research and developments of benzimidazole based medicinal chemistry has become a rapidly developing and increasingly active topic. Subsequently, for TB there is an urgent need for the development of new drug molecules with newer targets and with an alternative mechanism of action. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review we have collected published reports on this versatile core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic benzimidazole-based anti-TB drugs.189