Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.

摘要: Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the infectious disease responsible for highest number of deaths worldwide. Herein, 22 new N-oxide-containing compounds were synthesized followed in vitro and vivo evaluation their antitubercular potential against Mtb. Compound 8 was found to be most promising compound, with MIC90 values 1.10 6.62 μM active nonreplicating Mtb, respectively. Additionally, we carried out experiments confirm safety efficacy compound 8; orally bioavailable highly effective, leading a reduction Mtb undetectable levels mouse model infection. Microarray-based initial studies on mechanism action suggest that blocks translation. Altogether, these results indicate benzofuroxan derivative lead development novel chemical class drugs.