Title of article
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
Author/Authors
Jin Li، نويسنده , , Brian S. Bronk، نويسنده , , John P. Dirlam، نويسنده , , Alan E. Blize، نويسنده , , Peter Bertinato، نويسنده , , Burton H. Jaynes، نويسنده , , Anne Hickman، نويسنده , , Christine Miskell، نويسنده , , Usha A. Pillai، نويسنده , , Jay S. Tibbitts، نويسنده , , Michelle L. Haven، نويسنده , , Nicole L. Kolosko، نويسنده , , Chris J. Barry، نويسنده , , Tara B. Manion، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
1996
To page
1999
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.
Keywords
obesity , MTP
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797974
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