Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.

Abstract:

:Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization led to the development of 5-amino-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamides which were functional antagonists. Structural features which were important to activity included a 1,5-substitution pattern on the naphthalene ring; a sulfonamide NH with a pK value < 7; an amine, preferably with alkyl substituents, at the 5-position; and methyl groups on both the 3- and 4-positions of the isoxazole.

journal_name

J Med Chem

authors

Stein PD,Floyd DM,Bisaha S,Dickey J,Girotra RN,Gougoutas JZ,Kozlowski M,Lee VG,Liu EC,Malley MF

doi

10.1021/jm00008a013

subject

Has Abstract,Author List Incomplete

pub_date

1995-04-14 00:00:00

pages

1344-54

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

38

pub_type

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