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
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. [email protected]
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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