Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Eur J Med Chem. 2020 Jan 15:186:111893. doi: 10.1016/j.ejmech.2019.111893. Epub 2019 Nov 16.

Abstract

The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives.

Keywords: Anti-inflammatory; Antimicrobial; Antitumor; CNS agents; Derivatives; Pyrazolone.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Central Nervous System / drug effects
  • Chemistry, Pharmaceutical
  • Humans
  • Inflammation / drug therapy
  • Neoplasms / drug therapy*
  • Pyrazolones / chemistry
  • Pyrazolones / pharmacology*

Substances

  • Anti-Infective Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents
  • Pyrazolones