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 ,
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.
