1, 2, 4-Triazolo [4, 3-a] pyrazine derivatives with human renin inhibitory activity. 1. Synthesis and biological properties of alkyl alcohol and statine derivatives

DA Roberts, RH Bradbury, D Brown…

Index: Roberts, David A.; Bradbury, Robert H.; Brown, David; Faull, Alan; Griffiths, David; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2326 - 2334

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Citation Number: 10

Abstract

A series of 1, 2, 4-triazolo [4, 3-a] pyrazine derivatives with human renin inhibitory activity, which incorporate (1S, 2S)-2-amino-1, 3-dicyclohexyl-l-hydrox~ ropane, statine (Sta), and (3S, 4S)-4-amino-5-cyclohexyl-3-hydroxy-pentanoic acid (ACHPA) transition-state mimetics, have been prepared. Structure-activity relationships for renin inhibitory activity in the series are consistent with the 2-[8-isobutyl-6-phenyl-1, 2, 4-triazolo [4, 3-a] pyrazin-3-y1]-3-(3- ...