Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4, 5-dimethyl-3-isoxazolyl) amino] sulfonyl]-4-(2-oxazolyl)[1, 1'-biphenyl]-2-yl] methyl]-N, …

N Murugesan, Z Gu, S Spergel, M Young…

文献索引：Murugesan, Natesan; Gu, Zhengxiang; Spergel, Steven; Young, Marian; Chen, Ping; Mathur, Arvind; Leith, Leslie; Hermsmeier, Mark; Liu, Eddie C.-K.; Zhang, Rongan; Bird, Eileen; Waldron, Tom; Marino, Anthony; Koplowitz, Barry; Humphreys, W. Griffith; Chong, Saeho; Morrison, Richard A.; Webb, Maria L.; Moreland, Suzanne; Trippodo, Nick; Barrish, Joel C. Journal of Medicinal Chemistry, 2003 , vol. 46, # 1 p. 125 - 137

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被引用次数: 50

摘要

We have previously disclosed the selective ETA receptor antagonist N-(3, 4-dimethyl-5- isoxazolyl)-4'-(2-oxazolyl)[1, 1'-biphenyl]-2-sulfonamide (1, BMS-193884) as a clinical development candidate. Additional SAR studies at the 2'-position of 1 led to the identification of several analogues with improved binding affinity as well as selectivity for the ETA receptor. Following the discovery that a 3-amino-isoxazole group displays significantly ...