Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile

…, C Hutchins, JA Kester, JR Wu-Wong…

Index: Von Geldern, Thomas W.; Hutchins, Charles; Kester, Jeffrey A.; Wu-Wong, Jinshyun R.; Chiou, William; Dixon, Douglas B.; Opgenorth, Terry J. Journal of Medicinal Chemistry, 1996 , vol. 39, # 4 p. 957 - 967

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Citation Number: 34

Abstract

The pseudotetrapeptide FR-139317 is a potent and highly selective antagonist of the endothelin-A (ETA) receptor; however, its peptidic nature leads to poor oral absorption characteristics which make it an unlikely drug candidate. In an attempt to improve these properties, we have replaced a portion of the amide bond framework of FR-139317 with a heterocyclic surrogate. The resultant analogs are also ETA-selective antagonists, but ...

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