Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications

被引：19

作者：

McBriar, Mark D. ^{[1
]}

Guzik, Henry ^{[1
]}

Shapiro, Sherry ^{[1
]}

Xu, Ruo ^{[1
]}

Paruchova, Jaroslava ^{[1
]}

Clader, John W. ^{[1
]}

O'Neill, Kim ^{[1
]}

Hawes, Brian ^{[1
]}

Sorota, Steve ^{[1
]}

Margulis, Michael ^{[1
]}

Tucker, Kristal ^{[1
]}

Weston, Daniel J. ^{[1
]}

Cox, Kathleen ^{[1
]}

机构：

[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 16期

关键词：

melanin concentrating hormone; hERG; MCH; obesity;

D O I：

10.1016/j.bmcl.2006.05.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists for the hERG channel. This paper describes one of several strategies incorporated to limit hERG binding via modifications of a terminal aryl group in an otherwise promising bicyclohexyl urea series. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4262 / 4265

页数：4

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