Pyrazole scaffold-based derivatives: A glimpse of α-glucosidase inhibitory activity, SAR, and route of synthesis

Arch Pharm (Weinheim). 2023 May;356(5):e2200421. doi: 10.1002/ardp.202200421. Epub 2023 Jan 8.

Abstract

The α-glucosidase is a validated target to develop drugs for treating type 2 diabetes mellitus. The existing α-glucosidase inhibitors have certain shortcomings related to side effects and route of synthesis. Accordingly, it is inevitable to develop new chemical templates as α-glucosidase inhibitors. Pyrazole derivatives have a special place in medicinal chemistry because of various biological activities. Recently, pyrazole-based heterocyclic compounds have emerged as a promising scaffold to develop α-glucosidase inhibitors. This study focuses on the recently reported pyrazole-based α-glucosidase inhibitors, including their biological activity (in vivo, in vitro, and in silico), structure-activity relationship, and ways of synthesis. The literature revealed the development of several promising pyrazole-based α-glucosidase inhibitors and new synthetic routes for their preparation. The encouraging α-glucosidase inhibitory results of the pyrazole-based heterocyclic compounds make them an attractive target for further research. The authors also foresee the arrival of the pyrazole-based α-glucosidase inhibitors in clinical practice.

Keywords: biological activity; docking study; pyrazole; structure-activity relationship; α-glucosidase inhibitors.

Publication types

  • Review

MeSH terms

  • Diabetes Mellitus, Type 2* / drug therapy
  • Glycoside Hydrolase Inhibitors*
  • Humans
  • Molecular Docking Simulation
  • Molecular Structure
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology
  • Structure-Activity Relationship
  • alpha-Glucosidases / metabolism

Substances

  • Glycoside Hydrolase Inhibitors
  • alpha-Glucosidases
  • Pyrazoles