Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 5, 2009, Pages 1416-1420

  Vu, Chi B ^a   Milne, Jill C ^a   Carney, David P ^a   Song, Jeffrey ^a   Choy, Wendy ^a   Lambert, Philip D ^a   Gagne, David J ^a   Hirsch, Michael ^a   Cote, Angela ^a   Davis, Meghan ^a   Lainez, Elden ^a   Meade, Nekeya ^a   Normington, Karl ^a   Jirousek, Michael R ^a   Perni, Robert B ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; ANTIOBESITY AGENT; BENZOTHIAZOLE DERIVATIVE; CHOLESTEROL; DIRLOTAPIDE; GLUCOSE; INSULIN; MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN INHIBITOR; TRIACYLGLYCEROL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BODY WEIGHT; CELL STRAIN HEPG2; CHOLESTEROL BLOOD LEVEL; DISEASE MODEL; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG SPECIFICITY; DRUG STRUCTURE; ENZYME ASSAY; FOOD INTAKE; GLUCOSE HOMEOSTASIS; HUMAN; HUMAN CELL; IC 50; INSULIN SENSITIVITY; INTESTINE CELL; LIVER CELL; LIVER TOXICITY; MALE; MOUSE; NONHUMAN; OBESITY; OUTCOME ASSESSMENT; RAT; TRIACYLGLYCEROL BLOOD LEVEL; WEIGHT REDUCTION;

ANIMALS; BENZOTHIAZOLES; CARRIER PROTEINS; CELL LINE, TUMOR; DRUG DISCOVERY; ENTEROCYTES; HUMANS; MALE; MICE; MICE, INBRED C57BL; OBESITY; RATS; RATS, SPRAGUE-DAWLEY;

MUS;

EID: 60449115612     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.044     Document Type: Article

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15. Compounds 2, 15, and 16 showed oral activity only at 10 mg/kg. Compounds 17-21 were not orally active at 10 mg/kg.
16. The IV vehicle was 5% EtOH, 5% Cremophor, and 90% water.