期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 14, 页码 5001-5014出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.05.066
关键词
LXR antagonist; alpha-Glucosidase inhibitor; Thalidomide analog
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan
- Japan Society
Liver X receptor (LXR) alpha/beta dual agonists are candidate medicaments for the treatment of metabolic syndrome, because their biological actions include increasing cholesterol efflux mediated by LXR beta. However, their clinical application is currently limited by their enhancing effect on triglyceride (TG) synthesis mediated by LXR alpha. Combination of an LXR alpha-selective antagonist with an LXR alpha/beta dual agonist may overcome this disadvantage. In the present work, structural development studies of phenethylphenyl phthalimide 9, which possesses LXR alpha/beta dual-antagonistic activity and alpha-glucosidase-inhibitory activity, led to the LXR alpha-selective antagonist 23f. Specific alpha-glucosidase inhibitors were also obtained. (C) 2009 Elsevier Ltd. All rights reserved.
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