title: 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
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.
authors: Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. James.Li@bms.com
authors: James J
authors: JJ
authors: Li
authors: Haixia
authors: H
authors: Wang
authors: Joseph A
authors: JA
authors: Tino
authors: Jeffrey A
authors: JA
authors: Robl
authors: Timothy F
authors: TF
authors: Herpin
authors: R Michael
authors: RM
authors: Lawrence
authors: Scott
authors: S
authors: Biller
authors: Haris
authors: H
authors: Jamil
authors: Randy
authors: R
authors: Ponticiello
authors: Luping
authors: L
authors: Chen
authors: Ching-hsuen
authors: CH
authors: Chu
authors: Neil
authors: N
authors: Flynn
authors: Dong
authors: D
authors: Cheng
authors: Rulin
authors: R
authors: Zhao
authors: Bangchi
authors: B
authors: Chen
authors: Dora
authors: D
authors: Schnur
authors: Mary T
authors: MT
authors: Obermeier
authors: Vito
authors: V
authors: Sasseville
authors: Ramesh
authors: R
authors: Padmanabha
authors: Kristen
authors: K
authors: Pike
authors: Thomas
authors: T
authors: Harrity
mesh_terms: D001275:ATP Citrate (pro-S)-Lyase / Q000037:antagonists & inhibitors*; D000273:Adipose Tissue / Q000187:drug effects; D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001554:Benzene / Q000737:chemistry*; D001786:Blood Glucose / Q000032:analysis; D001835:Body Weight / Q000187:drug effects; D002478:Cells, Cultured; D002784:Cholesterol / Q000097:blood; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D051381:Rats; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood
chemical_list: D019440:Anti-Obesity Agents; D001786:Blood Glucose; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D014280:Triglycerides; D002784:Cholesterol; D001275:ATP Citrate (pro-S)-Lyase; D001554:Benzene