Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.

Journal of medicinal chemistry ·Vol. 39 ·No. 11 ·1996-05-24 ·Pages 2123-8

Riechers H, Albrecht HP, Amberg W, Baumann E, Bernard H, Böhm HJ, Klinge D, Kling A, Müller S, Raschack M, Unger L, Walker N, Wernet W

Abstract

A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.

MeSH Terms

Administration, Oral Animals Dansyl Compounds/pharmacology Death, Sudden Drug Design Endothelin Receptor Antagonists Endothelins/antagonists & inhibitors,toxicity Humans Ligands Models, Molecular Molecular Structure Pyrimidines/chemical synthesis,pharmacology Rats Receptor, Endothelin A Receptors, Endothelin/metabolism Structure-Activity Relationship Sulfonamides/pharmacology

Chemicals

Dansyl Compounds Endothelin Receptor Antagonists Endothelins Ligands Pyrimidines Receptor, Endothelin A Receptors, Endothelin Sulfonamides Ro 46-2005 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide

Authors & Affiliations

13 authors, click to expand affiliations / ORCID

Riechers H

Hauptlaboratorium, BASF AG, Ludwigshafen, Germany.

Albrecht H P

Amberg W

Baumann E

Bernard H

Böhm H J

Klinge D

Kling A

Müller S

Raschack M

Unger L

Walker N

Wernet W

Article Info

Journal

Journal of medicinal chemistry

Abbr.

J Med Chem

ISSN

0022-2623

DOI

10.1021/jm960274q

Published

1996-05-24

Pages

2123-8

Language

English

Region

United States

NLM ID

9716531

Subset

External Links

PubMed source DOI: 10.1021/jm960274q View journal details

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Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.

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