Design and synthesis of nonpeptide angiotensin II receptor antagonists featuring acyclic imidazole-mimicking structural units

Bioorg Med Chem. 1998 Nov;6(11):2013-27. doi: 10.1016/s0968-0896(98)00160-6.

Abstract

Extensive molecular modelling studies, including conformational analysis and the comparison of molecular electrostatic potential distributions, wee used to evaluate structural parameters of new antagonists containing acyclic replacements of the N = C-N imidazole region. The synthesis and the biological screening of a series of acyl biphenyltetrazole derivatives were planned and realized to gain an insight into the structure-activity relationships of this unusual class of Angiotensin II antagonists.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin Receptor Antagonists*
  • Antihypertensive Agents / chemistry
  • Biphenyl Compounds / chemical synthesis
  • Biphenyl Compounds / chemistry*
  • Biphenyl Compounds / pharmacology
  • Drug Design
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Imidazoles / pharmacology
  • Kinetics
  • Losartan / chemistry
  • Models, Molecular
  • Molecular Conformation
  • Molecular Structure
  • Static Electricity
  • Stereoisomerism
  • Structure-Activity Relationship
  • Tetrazoles / chemical synthesis
  • Tetrazoles / chemistry*
  • Tetrazoles / pharmacology
  • Valine / analogs & derivatives
  • Valine / chemistry
  • Valsartan

Substances

  • Angiotensin Receptor Antagonists
  • Antihypertensive Agents
  • Biphenyl Compounds
  • Imidazoles
  • Tetrazoles
  • Valsartan
  • Valine
  • Losartan