Heterocyclic isosters of antimycobacterial salicylanilides

Farmaco. 2005 May;60(5):399-408. doi: 10.1016/j.farmac.2005.02.002. Epub 2005 Apr 12.

Abstract

A series of 64 derivatives of substituted heterocyclic analogues of salicylanilides was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. For the QSAR study, the combination of Free-Wilson approach with Hansch approach was used. The molecules were separated on the heterocyclic and salicyl moieties and the study of influences of electronic and hydrophobic properties was used as well. The compounds are a new group of potential anti-tuberculotics.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Chemistry, Pharmaceutical / methods
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Microbial Sensitivity Tests / methods
  • Salicylamides / chemical synthesis*
  • Salicylamides / pharmacology

Substances

  • Anti-Bacterial Agents
  • Heterocyclic Compounds
  • Salicylamides