4.5 Article

2-Hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 11, Pages 3208-3211

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.03.017

Keywords

ATP-citrate lyase (ACL) inhibitors; lipid; glycemic profiles and weight loss.

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A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC50 = 0.13 mu M). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain. (C) 2007 Elsevier Ltd. All rights reserved.

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