DISCOVERY AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF SULFONAMIDE ETA-SELECTIVE ANTAGONISTS

Citation
Pd. Stein et al., DISCOVERY AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF SULFONAMIDE ETA-SELECTIVE ANTAGONISTS, Journal of medicinal chemistry, 38(8), 1995, pp. 1344-1354
Citations number
54
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry Medicinal
ISSN journal
0022-2623
Volume
38
Issue
8
Year of publication
1995
Pages
1344 - 1354
Database
ISI
SICI code
0022-2623(1995)38:8<1344:DASOSE>2.0.ZU;2-R
Abstract
Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization l ed to the development of 4-dimethyl-5-isoxazolyl)-1-naphthalenesulfona mides which were functional antagonists. Structural features which wer e important to activity included a 1,5-substitution pattern on the nap hthalene ring; a sulfonamide NH with a pK value < 7; an amine, prefera bly with alkyl substituents, at the 5-position; and methyl groups on b oth the 3- and 4-positions of the isoxazole.