Recent insight into the biological activities and SAR of quinolone derivatives as multifunctional scaffold

Bioorg Med Chem. 2022 Apr 1:59:116674. doi: 10.1016/j.bmc.2022.116674. Epub 2022 Feb 18.

Abstract

Quinolones are a type of bicyclic privileged building block with immense therapeutic potential. They are known for their crucial role in modulating numerous diseases conditions. In the present review, quinolone and its derivatives with different pharmacological properties like antibacterial, anticancer, anti-HIV, antitubercular and antimalarial activities are described on the basis of their structure activity relationship studies. Literature is mainly focused on the structural changes responsible for the significant increase in the therapeutic profile of the quinolone scaffold and its derivatives. The substitution pattern in the scaffold responsible for a substantial rise in the potency of specific activity has also been discussed, while emphasizing their potential as lead molecule for the drug discovery and development. Moreover, updates of recent research findings on this scaffold are also discussed.

Keywords: Biological activities; Quinolone; Scaffold; Structure–activity relationship.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Antimalarials* / pharmacology
  • Drug Discovery
  • Molecular Structure
  • Quinolones* / chemistry
  • Quinolones* / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Antimalarials
  • Quinolones