New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl …

RH Bradbury, C Bath, RJ Butlin, M Dennis…

Index: Bradbury, Robert H.; Bath, Colin; Butlin, Roger J.; Dennis, Michael; Heys, Christine; Hunt, Sarah J.; James, Roger; Mortlock, Andrew A.; Sumner, Neil F.; Tang, Eric K.; Telford, Berwick; Whiting, Elaine; Wilson, Campbell Journal of Medicinal Chemistry, 1997 , vol. 40, # 6 p. 996 - 1004

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Citation Number: 48

Abstract

Use of automated synthesis led to the discovery of several 6-membered nitrogen heterocycles as replacements for the N-isoxazolyl substituent present in the 1- naphthalenesulfonamide endothelin-A (ETA) antagonist 5-(dimethylamino)-N-(3, 4-dimethyl- 5-isoxazolyl)-1-naphthalenesulfonamide (BMS 182874). In each of these heterocycles, a small substituent such as halogen para to the position of attachment to the sulfonamide ...