Identification of a New Class of ET_A Selective Endothelin Antagonists by Pharmacophore Directed Screening

Autor:	Chan, M.F., Okun, I., Stavros, F.L., Hwang, E., Wolff, M.E., Balaji, V.N.
Zdroj:	Biochemical and Biophysical Research Communications; May 30, 1994, Vol. 201 Issue: 1 p228-234, 7p
Abstrakt:	Novel endothelin antagonists were identified through a "pharmacophore directed screening" strategy. The sulfanilamide antibacterial agent sulfisoxazole was found to be a good endothelin receptor antagonist (IC50's of 0.60 µM and 22 µM for the ETA and ETB receptors, respectively). The structurally similar sulfamethoxazole was found to be a weaker antagonist (IC50 for ETA 16 µM and for ETB 230 µM). These compounds represent a new class of low molecular weight and ETA-selective non-peptide endothelin antagonists.Copyright 1994, 1999 Academic Press, Inc.
Databáze:	Supplemental Index
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