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

…, P Bertinato, BH Jaynes, A Hickman, C Miskell…

文献索引：Li, Jin; Bronk, Brian S.; Dirlam, John P.; Blize, Alan E.; Bertinato, Peter; Jaynes, Burton H.; Hickman, Anne; Miskell, Christine; Pillai, Usha A.; Tibbitts, Jay S.; Haven, Michelle L.; Kolosko, Nicole L.; Barry, Chris J.; Manion, Tara B. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 7 p. 1996 - 1999

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被引用次数: 16

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 (3) 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.