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Endothelin receptor antagonists: synthesis and structure-activity relationships of substituted
K A Berryman1, J J Edmunds, A M Bunker
1Department of Chemistry, Parke-Davis Pharmaceutical Research, Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Bioorganic & Medicinal Chemistry
|November 5, 1998
Abstract:
The development of benzothiazine-1,1-dioxide derivatives as a new structural class of potent endothelin receptor antagonists is described. Structure-activity relationships (SAR) revealed that PD164800 (1) is a potent antagonist of the ETA receptor subtype.