Discovery and synthesis of a potent sulfonamide ETB selective antagonist

Autor:	Yasuhiko Kanda, Toshiro Konoike, Yoshitaka Araki, Shin-ichi Mihara, Masafumi Fujimoto, Tadashi Takahashi
Rok vydání:	2000
Předmět:	Endothelin Receptor Antagonists Stereochemistry Clinical Biochemistry Pharmaceutical Science Selective antagonist Biochemistry Chemical synthesis Muscle Smooth Vascular Cell Line Radioligand Assay Drug Discovery Animals Receptor Molecular Biology Aorta chemistry.chemical_classification Sulfonamides Endothelin Antagonists Molecular Structure Receptors Endothelin Organic Chemistry Antagonist Receptor Endothelin B In vitro Rats Sulfonamide chemistry COS Cells Molecular Medicine Endothelin receptor
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 10:1875-1878
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(00)00366-8
Popis:	The synthesis and structure–activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ET B selective antagonists. The most potent compound 15f displays IC 50 values of 1.7 μM and 0.002 μM to ET A and ET B receptors, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5399682ad71ee1ffa2708687046a08bd https://doi.org/10.1016/s0960-894x(00)00366-8 Zobrazit plný text záznamu Full Text from ScienceDirect