期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 14, 页码 2498-2503出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.05.055
关键词
Type 2 diabetes; ACC2 inhibitor; Olefin; Benzothiazole
Novel acetyl-CoA carboxylase 2 (ACC2) selective inhibitors were identified by the conversion of the alkyne unit of A-908292 to the olefin linker. Modification of the center and left part of the lead compound 1b improved the ACC2 inhibitory activity and CYP450 inhibition profile, and afforded a highly selective ACC2 inhibitor 2e which showed in vivo efficacy in C57BL/6 mice.
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