Oxetanes as promising modules in drug discovery

被引：187

作者：

Wuitschik, Georg

Rogers-Evans, Mark

Mueller, Klaus

Fischer, Holger

Wagner, Bjoern

Schuler, Franz

Polonchuk, Liudmila

Carreira, Erick M.

机构：

[1] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland

[2] Hoffmann La Roche Ag, Div Pharmaceut, Mol Properties & Struct Correlat Grp, CH-4070 Basel, Switzerland

[3] Hoffmann La Roche Ag, Div Pharmaceut, DMPK Dept, CH-4070 Basel, Switzerland

[4] Hoffmann La Roche Ag, Div Pharmaceut, Safety Pharmacol, CH-4070 Basel, Switzerland

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2006年 / 45卷 / 46期

关键词：

drug design; metabolism; oxetanes; small ring systems; synthesis design;

D O I：

10.1002/anie.200602343

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Chemical Equation Presented) Ring the changes: Introduction of an oxetane ring results in remarkably improved physico- and biochemical properties of the underlying scaffold. The oxetane ring confers enhanced solubility, reduces the metabolic degredation, lipophilicity, and amphiphilicity, and modulates the basicity of a nearby amine group. © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：7736 / 7739

页数：4

共 14 条

[1] SYNTHESIS OF ELECTRON-DEFICIENT OXETANES - 3-AZIDOOXETANE, 3-NITROOXETANE, AND 3,3-DINITROOXETANE [J].