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1. ChemInform Abstract: Synthesis and Structure-Activity Relationships of 9-Substituted Acridines as Endothelin-A Receptor Antagonists

Author

Annette Marian Doherty, Kathleen M. Welch, Chet Lee, S. Klutchko, R. Thomas Winters, Xue-Min Cheng, M. A. Flynn, and E. E. Reynolds

Subjects
Chemistry, Stereochemistry, cardiovascular system, Acridine derivatives, General Medicine, respiratory system, Selective antagonist, Endothelin receptor, Endothelin A Receptor Antagonists, circulatory and respiratory physiology
Abstract

Screening of a compound library against endothelin receptors (ETA and ETB) revealed PD 102566 (compound 1) as an ETA selective antagonist. Synthesis and structure-activity relationships (SAR) of a series of analogs are described.

Published
2010
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