Gerspacher, Marc, Altmann, Eva, Beerli, Rene, Buhl, Thomas, Endres, Ralf, Gamse, Rainer, Kameni Tcheudji, Jacques, Kneissel, Michaela, Krawinkler, Karl Heinz, Missbach, Martin, Schmidt, Alfred, Seuwen, Klaus, 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