Rational Design and Synthesis of AT1R Antagonists

Molecules. 2021 May 14;26(10):2927. doi: 10.3390/molecules26102927.

Abstract

Hypertension is one of the most common diseases nowadays and is still the major cause of premature death despite of the continuous discovery of novel therapeutics. The discovery of the Renin Angiotensin System (RAS) unveiled a path to develop efficient drugs to fruitfully combat hypertension. Several compounds that prevent the Angiotensin II hormone from binding and activating the AT1R, named sartans, have been developed. Herein, we report a comprehensive review of the synthetic paths followed for the development of different sartans since the discovery of the first sartan, Losartan.

Keywords: AT1R; Angiotensin II; hypertension; rational design; sartans.

Publication types

  • Review

MeSH terms

  • Angiotensin II Type 1 Receptor Blockers / chemical synthesis*
  • Angiotensin II Type 1 Receptor Blockers / chemistry
  • Animals
  • Drug Design*
  • Humans
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry
  • Receptor, Angiotensin, Type 1 / metabolism*

Substances

  • Angiotensin II Type 1 Receptor Blockers
  • Prodrugs
  • Receptor, Angiotensin, Type 1