Selective ETA antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives

…, B Porter, AG Roach, C Sargent, C Smith…

Index: Astles, Peter C.; Brown, Thomas J.; Halley, Frank; Handscombe, Caroline M.; Harris, Neil V.; Majid, Tahir N.; McCarthy, Clive; McLay, Lain M.; Morley, Andrew; Porter, Barry; Roach, Alan G.; Sargent, Carol; Smith, Christopher; Walsh, Roger J. A. Journal of Medicinal Chemistry, 2000 , vol. 43, # 5 p. 900 - 910

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Citation Number: 41

Abstract

The fifth paper in this series describes the culmination of our investigations into the development of a potent and selective ETA receptor antagonist for the treatment of diseases mediated by ET-1. Receptor site mapping of several ETA antagonists prepared previously identified a common cationic binding site which prompted synthesis of phenoxyphenylacetic acid derivative 13a, which showed good in vitro activity (IC50 59 nM, rat aortic ETA). ...