Author/Authors :
Ahmed S. Aboraia، نويسنده , , Sook Wah Yee، نويسنده , , Mohamed Sayed Gomaa، نويسنده , , Nikhil Shah، نويسنده , , Anna C. Robotham، نويسنده , , Bart Makowski، نويسنده , , David Prosser، نويسنده , , Andrea Brancale، نويسنده , , Glenville Jones، نويسنده , , Claire Simons، نويسنده ,
Abstract :
A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3–72 μM compared with the standard ketoconazole IC50 0.52 μM, with the styryl derivative (11c) displaying enhanced activity (IC50 = 0.3 μM) compared with the standard, providing a useful preliminary lead for drug development.
Keywords :
Benzofuran-2-carboxamides , CYP24A1 , Enzyme inhibition , molecular modelling , N-(2-(1H-Imidazol-1-yl)-2-phenylethyl)arylamides
