Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets

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 IC50 of 10−8 M order and good blood pressure lowering effects after oral administration to sodium-depleted marmosets.