Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design

作者：Pieroni Marco; Wan Baojie; Zuliani Valentina; Franzblau Scott G; Costantino Gabriele; Rivara Mirko

来源：European Journal of Medicinal Chemistry, 2015, 100: 44-49.

DOI：10.1016/j.ejmech.2015.05.048

• Tuberculosis
• Multidrug-resistance
• Imidazoles
• Latent tuberculosis
• Drug-repositioning

TB, caused by Mycobacterium tuberculosis, is one of the deadliest infections worldwide. The co-infection with HIV and the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) strains have further increased the burden for this disease. In the attempt to respond to the constant need of novel therapeutic options, we herein report the discovery of 2,4-diphenyl-1H-imidazoles as effective antitubercular agents, with MIC in the low micromolar range against actively replicating and persistent M. tuberculosis strains. The good activity, along with the lack of toxicity and the feasible synthesis, underscore their value as novel scaffolds for the development of new anti-TB drugs.

• 出版日期2015-7-15