期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 11, 页码 2539-2545出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.096
关键词
GPR119; Agonist; Type 2 diabetes
Through appropriate medicinal chemistry design tactics and computer-assisted conformational modeling, the initial lead A was evolved into a series of dihydrobenzofuran derivatives 3 as potent GPR119 agonists. This Letter describes the optimization of general structure 3, including the substituent(s) on dihydrobenzofuran, the R-1 attachment on right-hand piperidine nitrogen, and the left-hand piperidine/piperazine and its attachment R-2. The efforts led to the identification of compounds 13c and 24 as potent human GPR119 modulators with favorable metabolic stability, ion channel activity, and PXR profiles. (C) 2014 Elsevier Ltd. All rights reserved.
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