Renin inhibitory pentols showing improved enteral bioavailability

HW Kleemann, H Heitsch, R Henning…

Index: Kleemann, Heinz-Werner; Heitsch, Holger; Henning, Rainer; Kramer, Werner; Kocher, Walter; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 559 - 567

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Citation Number: 26

Abstract

Incorporation of a C-terminal pentahydroxy functionality led to potent, low molecular weight hydrophilic renin inhibitors lacking the P,'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 ...