1,3-DIARYL-2-CARBOXYINDOLES AS POTENT NONPEPTIDE ENDOTHELIN ANTAGONISTS

Authors
BUNKER AM EDMUNDS JJ BERRYMAN KA WALKER DM FLYNN MA WELCH KM DOHERTY AM
Citation
Am. Bunker et al., 1,3-DIARYL-2-CARBOXYINDOLES AS POTENT NONPEPTIDE ENDOTHELIN ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(9), 1996, pp. 1061-1066
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
9
Year of publication
1996
Pages
1061 - 1066
Database
ISI
SICI code
0960-894X(1996)6:9<1061:1APNEA>2.0.ZU;2-T
Abstract
Endothelin-1 is a potent vasoconstrictor that is thought to be involve d in many human disease states. We have developed a series of indole n on-peptide endothelin antagonists including PD 159110 (31), an ET(A) s elective antagonist, and PD 159020 (37), a non-selective ET(A)/ET(B) a ntagonist. The discovery, synthesis, and structure-activity relationsh ips of this series of compounds are described. (C) 1996 Elsevier Scien ce Ltd.