Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
Basic Information
ID: ALA1221312
Journal: Bioorg Med Chem Lett
Title: Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
Authors: Gerspacher M, Altmann E, Beerli R, Buhl T, Endres R, Gamse R, Kameni-Tcheudji J, Kneissel M, Krawinkler KH, Missbach M, Schmidt A, Seuwen K, Weiler S, Widler L.
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.
CiteXplore: 20685119
DOI: 10.1016/j.bmcl.2010.07.016
Patent ID: ┄