Discovery of 4′-[(imidazol-1-yl) methyl] biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists

…, MC Kowala, H Monshizadegan, N Murugesan…

Index: Tellew, John E; Baska, Rose Ann F; Beyer, Sophie M; Carlson, Kenneth E; Cornelius, Lyndon A; Fadnis, Leena; Gu, Zhengxiang; Kunst, Bridgette L; Kowala, Mark C; Monshizadegan, Hossain; Murugesan, Natesan; Ryan, Carol S; Valentine, Maria T; Yang, Yifan; Macor, John E Bioorganic and medicinal chemistry letters, 2003 , vol. 13, # 6 p. 1093 - 1096

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Citation Number: 15

Abstract

A series of 4′-[(imidazol-1-yl) methyl] biphenylsulfonamides has potent antagonist activity against both angiotensin II AT1 and endothelin ETA receptors. Such dual-acting antagonists could have utility in the treatment of hypertension, heart failure, and other cardiovascular diseases in a broad patient population. Certain compounds in the present series are orally active in a rat model of angiotensin II-mediated hypertension.