Document Report Card

ID: ALA1126155

Journal: J Med Chem

Title: Renin inhibitory pentols showing improved enteral bioavailability.

Authors: Kleemann HW, Heitsch H, Henning R, Kramer W, Kocher W, Lerch U, Linz W, Nickel WU, Ruppert D, Urbach H.

Abstract: Incorporation of a C-terminal pentahydroxy functionality led to potent, low molecular weight hydrophilic renin inhibitors lacking the P1' side chain. As these compounds are easy to synthesize and have sufficient water solubility, they were chosen for further study. Compound 33 was transported across rabbit intestinal brush border membrane vesicles and yielded a hypotensive effect in sodium-depleted rhesus monkeys which lasted for 90 min when dosed at 2 mg/kg id.

CiteXplore: 1738148

DOI: 10.1021/jm00081a019