Structure elucidation and conformational study of V8: a novel synthetic non peptide AT(1) antagonist

J Pharm Biomed Anal. 2006 Mar 18;40(5):1097-104. doi: 10.1016/j.jpba.2005.09.016. Epub 2005 Nov 2.

Abstract

AT(1) antagonists constitute the most recent class of antihypertensive drugs which act through the Renin Angiotensin System (RAS). In an effort to comprehend their stereoelectronic features, a study was initiated to compare the conformational properties of drugs already marketed for the treatment of hypertension with synthetic ones, possessing common structural characteristics. In this study, the synthetic AT(1) antagonist V8 is structurally elucidated and its conformational properties are studied through a combination of NMR spectroscopy and computational analysis. Its conformational properties are compared with those of the structurally similar prototype AT(1) antagonist losartan.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin II Type 1 Receptor Blockers / analysis
  • Angiotensin II Type 1 Receptor Blockers / chemistry*
  • Biphenyl Compounds / chemistry
  • Dimethyl Sulfoxide
  • Imidazoles / chemistry
  • Losartan / analogs & derivatives*
  • Losartan / analysis
  • Losartan / chemistry
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Conformation
  • Monte Carlo Method
  • Tetrazoles / chemistry

Substances

  • Angiotensin II Type 1 Receptor Blockers
  • Biphenyl Compounds
  • Imidazoles
  • Tetrazoles
  • V8 compound
  • Losartan
  • Dimethyl Sulfoxide