TB Research

Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents

Wang A, Lv K, Li L, Liu H, Tao Z, Wang B, Liu M, Ma C, et al. (12 authors)

European journal of medicinal chemistry · 2019-06

Abstract

A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates. Compounds 15b and 15d display good safety and pharmacokinetic profiles, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.

MeSH terms

  • Animals
  • Mice, Inbred ICR
  • Mice
  • Mycobacterium tuberculosis
  • Imidazoles
  • Pyridines
  • Antitubercular Agents
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship
  • Dose-Response Relationship, Drug
  • Drug Design
  • Female