Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists

HC Huang, DB Reitz, TS Chamberlain…

Index: Huang, Horng-Chih; Reitz, David B.; Chamberlain, Timothy S.; Olins, Gillian M.; Corpus. Valerie M.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 15 p. 2172 - 2181

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Citation Number: 24

Abstract

2, 5-Dibutyl-2, 4-dihydro-4-[[2-(1H-tetrazol-5-~ 1)[l, l'-biphenyl]-4'-yllmethyl]-3H-1, 2, 4-triazol- 3-one, SC-51316, was synthesized as a potent and orally active angiotensin I1 (AII) receptor antagonist with a long duration of action. To explore the lipophilic pocket in the AI1 receptor interacting with the substituent at the 2-position of triazolone-based antagonists, a series of compounds were prepared and evaluated for receptor binding affinity and antagonism of ...