Oxadiazole scaffolds in anti-tuberculosis drug discovery

Bioorg Med Chem Lett. 2019 Aug 15;29(16):1999-2007. doi: 10.1016/j.bmcl.2019.06.054. Epub 2019 Jun 28.

Abstract

With the increasing number of cases of latent and drug resistant tuberculosis, there is an urgent need to develop new, potent molecules capable of combating this deadly disease. Molecules containing oxadiazoles are one such class that could be considered to fulfil this need. Oxadiazole regioisomers have been explored in drug discovery programs for their ability to act as effective linkers and also as pharmacophoric features. Oxadiazoles can act as bioisosteric replacements for the hydrazide moiety which can be found in first line anti-TB drugs, and some have been also reported to interact with newer anti-TB targets. In this context, the present review describes the potential of oxadiazoles as antituberculosis agents.

Keywords: Bioisoster; Linker; Oxadiazole; Regioisomer; Tuberculosis.

Publication types

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

MeSH terms

  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Cell Line, Tumor
  • Drug Design
  • Drug Discovery
  • Humans
  • Isomerism
  • Mycobacterium tuberculosis / drug effects
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antitubercular Agents
  • Oxadiazoles