RENIN INHIBITORY PENTOLS SHOWING IMPROVED ENTERAL BIOAVAILABILITY

被引：29

作者：

KLEEMANN, HW

HEITSCH, H

HENNING, R

KRAMER, W

KOCHER, W

LERCH, U

LINZ, W

NICKEL, WU

RUPPERT, D

URBACH, H

UTZ, R

WAGNER, A

WECK, R

WIEGAND, F

机构：

[1] Hoechst AG, 6230 Frankfurt/M. 80

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 03期

关键词：

D O I：

10.1021/jm00081a019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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收藏

页码：559 / 567

页数：9

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