TB Research

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