Design, Synthesis, and Antibacterial Evaluation of Hybrid Product of Benzimidazole and Isoxazole.

A rapid and efficient method for synthesizing 1-[(3-aryl-5-isoxazolyl)methyl]-2-aryl-1H-benzimidazole was developed using 3-aryl-5-bromomethyl isoxazole and 2-substituted benzimidazoles as raw materials, which could be expanded to a wide range of benzimidazoles in moderate to excellent yields. Halo and hetero functional groups as well as alkyl groups were tolerated in this transformation. The antimycobacterial activity of all synthesized compounds were tested using rifampicin as a positive control. Some compounds exhibited moderate to good tuberculostatic activities against Mycobacteria smegmatis MC2155 with MIC values ranging from 64.00 to 128.00 µg/mL, providing lead compound for the subsequent development of anti-tuberculosis drugs.