2. Academic Validation
  3. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors

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

  • Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. doi: 10.1016/j.bmcl.2007.03.017.
James J Li 1,  Haixia Wang,  Joseph A Tino,  Jeffrey A Robl,  Timothy F Herpin,  R Michael Lawrence,  Scott Biller,  Haris Jamil,  Randy Ponticiello,  Luping Chen,  Ching-hsuen Chu,  Neil Flynn,  Dong Cheng,  Rulin Zhao,  Bangchi Chen,  Dora Schnur,  Mary T Obermeier,  Vito Sasseville,  Ramesh Padmanabha,  Kristen Pike,  Thomas Harrity
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. James.Li@bms.com
PMID: 17383874 DOI: 10.1016/j.bmcl.2007.03.017
Abstract

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 (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma Cholesterol, triglyceride, and glucose, as well as inhibited weight gain.

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