1,3-Disubstituted isoindolines have been discovered as a new class of poten
t functional ETA selective receptor antagonists through pharmacophore analy
sis of existing nonpeptide endothelin antagonists. The structure-activity r
elationships for both the trans and the tis series of isoindolines are disc
ussed. (C) 2001 Elsevier Science Ltd. All rights reserved.