Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and …

N Murugesan, Z Gu, L Fadnis, JE Tellew…

Index: Murugesan, Natesan; Gu, Zhengxiang; Fadnis, Leena; Tellew, John E.; Baska, Rose Ann F.; Yang, Yifan; Beyer, Sophie M.; Monshizadegan, Hossain; Dickinson, Kenneth E.; Valentine, Maria T.; Humphreys, W. Griffith; Lan, Shih-Jung; Ewing, William R.; Carlson, Kenneth E.; Kowala, Mark C.; Zahler, Robert; Macor, John E. Journal of Medicinal Chemistry, 2005 , vol. 48, # 1 p. 171 - 179

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Citation Number: 57

Abstract

In a previous report we demonstrated that merging together key structural elements present in an AT1 receptor antagonist (1, irbesartan) with key structural elements in a biphenylsulfonamide ETA receptor antagonist (2) followed by additional optimization provided compound 3 (Figure 1) as a dual-action receptor antagonist (DARA), which potently blocked both AT1 and ETA receptors. Described herein are our efforts directed ...