Piperidine-renin inhibitors compounds with improved physicochemical properties

被引：67

作者：

Güller, R ^{[1
]}

Binggeli, A ^{[1
]}

Breu, V ^{[1
]}

Bur, D ^{[1
]}

Fischli, W ^{[1
]}

Hirth, G ^{[1
]}

Jenny, C ^{[1
]}

Kansy, M ^{[1
]}

Montavon, F ^{[1
]}

Müller, M ^{[1
]}

Oefner, C ^{[1
]}

Stadler, H ^{[1
]}

Vieira, E ^{[1
]}

Wilhelm, M ^{[1
]}

Wostl, W ^{[1
]}

Märki, HP ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Pharma Res Dept, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(99)00196-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1403 / 1408

页数：6

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