In vitro and in vivo profile of 5-[(4′-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity

详细信息	查看全文 | 推荐本文 |

• 作者：Jin Li ; Brian S. Bronk ; John P. Dirlam ; Alan E. Blize ; Peter Bertinato ; Burton H. Jaynes ; Anne Hickman ; Christine Miskell ; Usha A. Pillai ; Jay S. Tibbitts ; et al.
• 关键词：MTP ; Obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 April 2007
• 卷：17
• 期：7
• 页码：1996-1999
• 文件大小：135 K

摘要

The synthesis of a novel gut selective MTP inhibitor, 5-[(4′-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), and its in vitro and in vivo profile are described. Dirlotapide (trong>3trong>) demonstrated excellent potency against MTP enzyme in HepG2 cells and canine hepatocytes. This novel MTP inhibitor also showed excellent efficacy when tested in a canine food intake model.