Design, synthesis and evaluation of oxime-functionalized nitrofuranylamides as novel antitubercular agents
Fan YL, Wu JB, Ke X, Huang ZP
Bioorganic & medicinal chemistry letters · 2018-08
Abstract
A series of oxime-functionalized nitrofuranylamides were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and drug-resistant clinical isolates. Among them, two compounds 7a and 7b exhibited excellent activity against the three tested strains. Both of them were comparable to the first-line anti-TB agents INH and RIF against MTB H37Rv, and were far more potent than INH and RIF against MDR-TB 16833 and 16995 strains. Thus, both of them could act as leads for further optimization.
MeSH terms
- Mycobacterium tuberculosis
- Amides
- Oximes
- Nitro Compounds
- Antitubercular Agents
- Microbial Sensitivity Tests
- Molecular Structure
- Structure-Activity Relationship
- Dose-Response Relationship, Drug
- Drug Design