Design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties
Wang A, Huang G, Wang B, Lv K, Wang H, Tao Z, Liu M, Guo H, et al. (9 authors)
Bioorganic & medicinal chemistry letters · 2018-07
Abstract
We report herein the design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties. Results reveal that many of the target compounds have considerable in vitro antitubercular activity. Especially, N-((2-(4-fluorophenyl)/N-((2-(3-fluorobenzyl)-1,2,3,4-tetrahydroisoquilin-6-yl)methyl)-3,5-dinitrobenzamides 18a and 20e exhibit potent MIC values of 0.056-0.078 μg/mL against both drug-sensitive Mycobacterium tuberculosis (MTB) H37Rv strain and two clinically isolated multidrug-resistant MTB (MDR-MTB) strains, opening a new direction for further SAR studies.
MeSH terms
- Mycobacterium tuberculosis
- Benzamides
- Anti-Bacterial Agents
- Microbial Sensitivity Tests
- Molecular Structure
- Structure-Activity Relationship
- Dose-Response Relationship, Drug
- Drug Design