THE DESIGN, BINDING-AFFINITY PREDICTION AND SYNTHESIS OF MACROCYCLIC ANGIOTENSIN-II AT(1) AND AT(2) RECEPTOR ANTAGONISTS

Authors
DELASZLO SE GLINKA TW GREENLEE WJ BALL R NACHBAR RB PRENDERGAST K
Citation
Se. Delaszlo et al., THE DESIGN, BINDING-AFFINITY PREDICTION AND SYNTHESIS OF MACROCYCLIC ANGIOTENSIN-II AT(1) AND AT(2) RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(8), 1996, pp. 923-928
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
8
Year of publication
1996
Pages
923 - 928
Database
ISI
SICI code
0960-894X(1996)6:8<923:TDBPAS>2.0.ZU;2-L
Abstract
Analysis of the SAR of AT(1) selective and AT(1)/AT(2) balanced affini ty angiotensin II antagonists led to the design of macrocyclic quinazo linone ligands. CoMFA analysis was used to predict the binding affinit ies of these novel ligands. The synthesis, X-ray crystal structure, bi nding affinity and the relevance of these studies to the determination of the biologically relevant binding conformation is discussed. Copyr ight (C) 1996 Elsevier Science Ltd