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

✍ Scribed by Marc Gerspacher; Eva Altmann; René Beerli; Thomas Buhl; Ralf Endres; Rainer Gamse; Jacques Kameni-Tcheudji; Michaela Kneissel; Karl Heinz Krawinkler; Martin Missbach; Alfred Schmidt; Klaus Seuwen; Sven Weiler; Leo Widler

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 784 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.016

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✦ Synopsis

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.

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