Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides
- Aboraia, Ahmed S.
- Yee, Sook Wah
- Gomaa, Mohamed Sayed
- Shah, Nikhil
- Robotham, Anna C.
- Makowski, Bart
- Prosser, David
- Brancale, Andrea
- Jones, Glenville
- Simons, Claire
DOIAbstract
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
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