• Title of article

    Novel acyl coenzyme A (CoA): Diacylglycerol acyltransferase-1 inhibitors: Synthesis and biological activities of diacylethylenediamine derivatives Original Research Article

  • Author/Authors

    Yoshihisa Nakada، نويسنده , , Thomas D. Aicher، نويسنده , , Yvan Le Huérou، نويسنده , , Timothy Turner، نويسنده , , Scott A. Pratt، نويسنده , , Stephen S. Gonzales، نويسنده , , Steve A. Boyd، نويسنده , , Hiroshi Miki، نويسنده , , Toshihiro Yamamoto، نويسنده , , Hiroshi Yamaguchi، نويسنده , , Koki Kato، نويسنده , , Shuji Kitamura، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2010
  • Pages
    11
  • From page
    2785
  • To page
    2795
  • Abstract
    A series of diacylethylenediamine derivatives were synthesized and evaluated for their inhibitory activity against DGAT-1 and pharmacokinetic profile to discover new small molecule DGAT-1 inhibitors. Among the compounds, N-[2-({[1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]carbonyl}amino)ethyl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide 3x showed potent inhibitory activity and excellent PK profile. Oral administration of 3x to mice with dietary-induced obesity resulted in reduced body weight gain and white adipose tissue weight.
  • Keywords
    DGAT-1 inhibitor , Inhibition of triacylglycerol synthesis , diet-induced obesity
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    2010
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1307284

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=1307284