Alpha-amylase as molecular target for treatment of diabetes mellitus: A comprehensive review

Chem Biol Drug Des. 2021 Oct;98(4):539-560. doi: 10.1111/cbdd.13909. Epub 2021 Jul 4.

Abstract

The alpha (α)-amylase is a calcium metalloenzyme that aids digestion by breaking down polysaccharide molecules into smaller ones such as glucose and maltose. In addition, the enzyme causes postprandial hyperglycaemia and blood glucose levels to rise. α-Amylase is a well-known therapeutic target for the treatment and maintenance of postprandial blood glucose elevations. Various enzymatic inhibitors, such as acarbose, miglitol and voglibose, have been found to be effective in targeting this enzyme, prompting researchers to express an interest in developing potent alpha-amylase inhibitor molecules. The review mainly focused on designing different derivatives of drug molecules such as benzofuran hydrazone, indole hydrazone, spiroindolone, benzotriazoles, 1,3-diaryl-3-(arylamino) propan-1-one, oxadiazole and flavonoids along with their target-receptor interactions, IC50 values and other biological activities.

Keywords: alpha-amylase; alpha-amylase inhibitors; antidiabetic drug; diabetes mellitus; molecular target.

Publication types

  • Review

MeSH terms

  • 1-Deoxynojirimycin / analogs & derivatives
  • 1-Deoxynojirimycin / chemistry
  • Acarbose / chemistry
  • Benzofurans / chemistry
  • Blood Glucose / drug effects
  • Diabetes Mellitus / drug therapy*
  • Drug Discovery
  • Flavonoids / chemistry
  • Glycoside Hydrolase Inhibitors / chemistry*
  • Glycoside Hydrolase Inhibitors / pharmacology
  • Humans
  • Hydrazones / chemistry
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / pharmacology
  • Indoles / chemistry
  • Inositol / analogs & derivatives
  • Inositol / chemistry
  • Oxadiazoles / chemistry
  • Structure-Activity Relationship
  • alpha-Amylases / metabolism*

Substances

  • Benzofurans
  • Blood Glucose
  • Flavonoids
  • Glycoside Hydrolase Inhibitors
  • Hydrazones
  • Hypoglycemic Agents
  • Indoles
  • Oxadiazoles
  • miglitol
  • 1-Deoxynojirimycin
  • Inositol
  • indole
  • alpha-Amylases
  • benzofuran
  • voglibose
  • Acarbose