Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists)

被引：9

作者：

Gerspacher, Marc ^{[1
]}

Altmann, Eva ^{[1
]}

Beerli, Rene ^{[1
]}

Buhl, Thomas ^{[1
]}

Endres, Ralf ^{[1
]}

Gamse, Rainer ^{[1
]}

Kameni-Tcheudji, Jacques ^{[1
]}

Kneissel, Michaela ^{[1
]}

Krawinkler, Karl Heinz ^{[1
]}

Missbach, Martin ^{[1
]}

Schmidt, Alfred ^{[1
]}

Seuwen, Klaus ^{[1
]}

Weiler, Sven ^{[1
]}

Widler, Leo ^{[1
]}

机构：

[1] Novartis Pharma AG, Novartis Inst BioMed Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 17期

关键词：

Calcium-sensing receptor (CaSR); Parathyroid hormone (PTH); Bone formation; Osteoporosis; CaSR-antagonist; Benzimidazoles; BONE;

D O I：

10.1016/j.bmcl.2010.07.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel benzimidazole derivatives has been designed via a scaffold morphing approach based on known calcilytics chemotypes. Subsequent lead optimisation led to the discovery of penta-substituted benzimidazoles that exhibit attractive in vitro and in vivo calcium-sensing receptor (CaSR) inhibitory profiles. In addition, synthesis and structure-activity relationship data are provided. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5161 / 5164

页数：4

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