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

Article abstract of DOI:10.1016/S0960-894X(97)00323-5

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.