Bioorganic and Medicinal Chemistry Letters p. 5161 - 5164 (2010)
Update date:2022-08-02
Topics:
Gerspacher, Marc
Altmann, Eva
Beerli, René
Buhl, Thomas
Endres, Ralf
Gamse, Rainer
Kameni-Tcheudji, Jacques
Kneissel, Michaela
Krawinkler, Karl Heinz
Missbach, Martin
Schmidt, Alfred
Seuwen, Klaus
Weiler, Sven
Widler, Leo
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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