DISCOVERY OF SUBSTITUTED 8,9-DICARBOXYLDIBENZO [2,35,6] BICYCLO [5.2.0] NONAN-4-ONES WITH MODERATE BINDING-AFFINITY TO THE ENDOTHELIN ET(A)AND ET(B) RECEPTORS

Authors
RIVERO RA GREENLEE WJ WILLIAMS PD KIECZYKOWSKI GR WILLIAMS DL
Citation
Ra. Rivero et al., DISCOVERY OF SUBSTITUTED 8,9-DICARBOXYLDIBENZO [2,35,6] BICYCLO [5.2.0] NONAN-4-ONES WITH MODERATE BINDING-AFFINITY TO THE ENDOTHELIN ET(A)AND ET(B) RECEPTORS, Bioorganic & medicinal chemistry letters, 5(13), 1995, pp. 1401-1404
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
13
Year of publication
1995
Pages
1401 - 1404
Database
ISI
SICI code
0960-894X(1995)5:13<1401:DOS8[B>2.0.ZU;2-X
Abstract
Screening of our sample collection for novel structures with endotheli n receptor (ET(A) and ET(B)) binding affinity, resulted in the discove ry of structure I (R = H). This unique bicyclic diacid elicited modest affinity for both cloned human receptors (0.8 mu M, ET(A) and 7.9 mu M, ET(B)). Substitution at 'R' resulted in increased affinity for both receptors.