Novel acyl coenzyme A (CoA): Diacylglycerol acyltransferase-1 inhibitors: Synthesis and biological activities of diacylethylenediamine derivatives
Y Nakada, TD Aicher, Y Le Huerou, T Turner… - Bioorganic & medicinal …, 2010 - Elsevier
Y Nakada, TD Aicher, Y Le Huerou, T Turner, SA Pratt, SS Gonzales, SA Boyd, H Miki…
Bioorganic & medicinal chemistry, 2010•ElsevierA 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 …
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 …
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.
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