Recent advances of pyrazole-containing derivatives as anti-tubercular agents

Eur J Med Chem. 2017 Oct 20:139:429-440. doi: 10.1016/j.ejmech.2017.07.059. Epub 2017 Aug 3.

Abstract

One-third of the world's population infected tuberculosis (TB), and more than 1 million deaths annually. The co-infection between the mainly pathogen Mycobacterium tuberculosis (MTB) and HIV, and the incidence of drug-resistant TB, multi-drug resistant TB, extensively drug-resistant TB as well as totally drug-resistant TB have further aggravated the mortality and spread of this disease. Thus, there is an urgent need to develop novel anti-TB agents against both drug-susceptible and drug-resistant TB. The wide spectrum of biological activities and successful utilization of pyrazole-containing drugs in clinic have inspired more and more attention towards this kind of heterocycles. Numerous of pyrazole-containing derivatives have been synthesized for searching new anti-TB agents, and some of them showed promising potency and may have novel mechanism of action. This review aims to outline the recent achievements in pyrazole-containing derivatives as anti-TB agents and their structure-activity relationship.

Keywords: Anti-mycobacterial activity; Anti-tuberculosis activity; Hybrid compounds; Pyrazole derivatives; Structure-activity relationship.

Publication types

  • Review

MeSH terms

  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Structure-Activity Relationship
  • Tuberculosis / drug therapy*

Substances

  • Antitubercular Agents
  • Pyrazoles
  • pyrazole