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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 |
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| Authors: | 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 |
| Institution: | Pfizer Inc., Groton, CT 06340, USA. jin.li@pfizer.com |
| Abstract: | 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. |
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