2-羟基-N-芳基苯磺酰胺作为ATP-柠檬酸裂解酶抑制剂
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
作者信息
Li James J, Wang Haixia, Tino Joseph A, Robl Jeffrey A, Herpin Timothy F, Lawrence R Michael, Biller Scott, Jamil Haris, Ponticiello Randy, Chen Luping, Chu Ching-hsuen, Flynn Neil, Cheng Dong, Zhao Rulin, Chen Bangchi, Schnur Dora, Obermeier Mary T, Sasseville Vito, Padmanabha Ramesh, Pike Kristen, Harrity Thomas
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. doi: 10.1016/j.bmcl.2007.03.017. Epub 2007 Mar 12.
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.
一系列新型的2-羟基-N-芳基苯磺酰胺被鉴定为ATP-柠檬酸裂解酶（ACL）抑制剂，其中化合物9表现出强大的体外活性（IC(50)=0.13 microM）。在高脂喂养的小鼠中对化合物9进行慢性口服给药可降低血浆胆固醇、甘油三酯和葡萄糖水平，并抑制体重增加。
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