Abstract

A series of low molecular renin inhibitors (molecular weight ∗< 600) were prepared and their biological activities were evaluated. The inhibitors containing indole-2-carbonyl moieties at the P3 position and 2-amino-3,5- anti -diol fragment at the P1-P1′ position showed renin inhibitory activities with IC 50 of 10 −8 M order and good blood pressure lowering effects after oral administration to sodium-depleted marmosets. A series of low molecular renin inhibitors (molecular weight ∗< 600) were prepared and their biological activities were evaluated.

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