Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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

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

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Article Details

VOLUME: 2
ISSUE: 8
Year: 2005
Page: [571 - 578]
Pages: 8
DOI: 10.2174/157018005774717325
Price: $58