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

August 14, 2017 | Autor: Peter Bertinato | Categoría: Organic Chemistry, Medicinal Chemistry, Obesity, Pharmacokinetics, Pharmaceutical Chemistry, Dogs, Cell line, In Vitro, Humans, Models, Animals, Drug Design, Enzyme, Food intake, In Vivo, Rats, Rat, Carboxylic Acids, Molecular Conformation, Bioorganic and medicinal Chemistry, Hydrogen-Ion Concentration, Chemical Synthesis, Carbamates, Selectivity, Dogs, Cell line, In Vitro, Humans, Models, Animals, Drug Design, Enzyme, Food intake, In Vivo, Rats, Rat, Carboxylic Acids, Molecular Conformation, Bioorganic and medicinal Chemistry, Hydrogen-Ion Concentration, Chemical Synthesis, Carbamates, Selectivity

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2007

Medicinal chemistry V 1100 In vitro and in vivo Profile of 5-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)-amiAcid Benzylmethyl Carbamoylamide (Dirlotapide), a 33- 229 no]-1H-indole-2-carboxylic Novel Potent MTP Inhibitor for Obesity. — Dirlotapide (I), obtained through a three-step linear synthesis, is a potent inhibitor of MTP, demonstrated by inhibition of Apo B secretion from human HepG2 cells and in canine hepatocytes. Its robust efficacy is shown in a food intake model. The unique ADME properties of (I) minimize the drug exposure providing a better safety profile. — (LI*, J.; et al.; Bioorg. Med. Chem. Lett. 17 (2007) 7, 1996-1999; Pfizer Inc., Groton, CT 06340, USA; Eng.) — H. Hoennerscheid

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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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