Renin inhibitors containing a pyridyl amino diol derived C-terminus

H Heitsch, R Henning, HW Kleemann…

文献索引：Heitsch; Henning; Kleemann; Linz; Nickel; Ruppert; Urbach; Wagner Journal of Medicinal Chemistry, 1993 , vol. 36, # 19 p. 2788 - 2800

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被引用次数: 25

摘要

Based on the concept of transition-state analogs, a series of nonpeptide renin inhibitors with the new (2S, 3R, 4S)-2-amino-l-cyclohexyl-3, 4-dihydroxy-6-(2-pyridyl) hexane moiety at the C-terminal functionality were synthesized and evaluated for inhibition of renin both in vitro and in vivo. All compounds exhibited potencies in the nanomolar or even subnanomolar range when tested versus human renin in vitro. Selected inhibitors were evaluated in ...