Rational Design of the New Antihypertensive I1-Receptor Ligand 2-(2- Biphenyl-2-yl-1-methyl-ethyl)-4,5-dihydro-1H-imidazole

F. Gentili; P. Bousquet; A. Carrieri; J. Feldman; F. Ghelfi; M. Giannella; A. Piergentili; W. Quaglia; C. Vesprini; M. Pigini

doi:10.2174/157018005774717325

Abstract

The new antihypertensive I1-receptor agonist (4) was rationally synthetized by the insertion of a phenyl group in the ortho position of the aromatic ring of the I1-selective antagonist (3). This "antagonismagonism" modulation, highlights the existence of expected analogies between I1- and α2-adrenoreceptor systems. Chirality proves to be crucial for the activation of I1-receptors, since the cardiovascular effects are produced exclusively by the (S)-(+)-4 enantiomer.

Keywords: Antihypertensive activity, I1-ligands, antagonism/agonism, molecular superposition

Rights & Permissions Print Cite

Letters in Drug Design & Discovery

Title: Rational Design of the New Antihypertensive I1-Receptor Ligand 2-(2- Biphenyl-2-yl-1-methyl-ethyl)-4,5-dihydro-1H-imidazole

Volume: 2 Issue: 8

Author(s): F. Gentili, P. Bousquet, A. Carrieri, J. Feldman, F. Ghelfi, M. Giannella, A. Piergentili, W. Quaglia, C. Vesprini and M. Pigini

Affiliation:

Keywords: Antihypertensive activity, I1-ligands, antagonism/agonism, molecular superposition

Abstract: The new antihypertensive I1-receptor agonist (4) was rationally synthetized by the insertion of a phenyl group in the ortho position of the aromatic ring of the I1-selective antagonist (3). This "antagonismagonism" modulation, highlights the existence of expected analogies between I1- and α2-adrenoreceptor systems. Chirality proves to be crucial for the activation of I1-receptors, since the cardiovascular effects are produced exclusively by the (S)-(+)-4 enantiomer.

Export Options

Export File:

RIS (for EndNote, Reference Manager, ProCite)

BibTeX

Text

Content:

Citation Only

Citation and Abstract

About this article

Cite this article as:

F. Gentili , P. Bousquet , A. Carrieri , J. Feldman , F. Ghelfi , M. Giannella , A. Piergentili , W. Quaglia , C. Vesprini and M. Pigini , Rational Design of the New Antihypertensive I1-Receptor Ligand 2-(2- Biphenyl-2-yl-1-methyl-ethyl)-4,5-dihydro-1H-imidazole, Letters in Drug Design & Discovery 2005; 2 (8) . https://dx.doi.org/10.2174/157018005774717325