Antituberculosis agents bearing the 1,2-disubstituted benzimidazole scaffold

作者:Yeong Keng Yoon*; Ang Chee Wei; Ali Mohamed Ashraf; Osman Hasnah; Tan Soo Choon
来源:Medicinal Chemistry Research, 2017, 26(4): 770-778.
DOI:10.1007/s00044-017-1784-2

摘要

The emergence of drug-resistant strains in recent years has fueled the epidemic of tuberculosis. This necessitates the development of new chemical scaffolds to curb resistant tuberculosis for effective control of this disease. In this study, we have designed and synthesized two series of benzimidazole derivatives. Their antimycobacterial activities were initially evaluated using Mycobacterium tuberculosis H37RV strains. The most potent analog (6h) was further assessed using various drug-resistant M. tuberculosis strains. This report described the importance of benzimidazoles as new antitmycobacterial agents targeting both the M. tuberculosis H37RV as well as the drug-resistant-tuberculosis strains. The trifluoromethyl group which was essential for antimycobacterial activity was also highlighted.

  • 出版日期2017-4