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Penta-Substituted Benzimidazoles as Potent Antagonists of the Calcium Sensing Receptor (CaSR-Antagonists)

Gerspacher, Marc and Altmann, Eva and Beerli, Rene and Buhl, Thomas and Endres, Ralf and Gamse, Rainer and Kameni Tcheudji, Jacques and Kneissel, Michaela and Krawinkler, Karl Heinz and Missbach, Martin and Schmidt, Alfred and Seuwen, Klaus and Weiler, Sven and Widler, Leo (2010) Penta-Substituted Benzimidazoles as Potent Antagonists of the Calcium Sensing Receptor (CaSR-Antagonists). Bioorganic & Medicinal Chemistry Letters.

Abstract

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.

Item Type: Article
Keywords: Calcium sensing receptor, antagonists, parathyroid hormone, osteoporosis, bone anabolic
Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/2814

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