期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 17, 页码 5161-5164出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.016
关键词
Calcium-sensing receptor (CaSR); Parathyroid hormone (PTH); Bone formation; Osteoporosis; CaSR-antagonist; Benzimidazoles
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. (C) 2010 Elsevier Ltd. All rights reserved.
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