期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 7, 页码 1228-1233出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.02.044
关键词
GPR119 agonist; Spirocyclic structure; Type 2 diabetes
Exploration of alternative structures of the substituted piperidine or piperazine ring which are characteristic in most of the reported GPR119 agonists provided novel spirocyclic cyclohexane derivatives. The representative 17 with a high three-dimensionality exhibited potent agonistic activity (EC50 = 4 nM) with no CYP inhibitory activity (IC50 > 10 mu M). Compound 17 also displayed hypoglycemic activity with insulin secretion dependent on glucose concentration in an intraperitoneal glucose tolerance test in rats. (C) 2018 Elsevier Ltd. All rights reserved.
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