Title of article
Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides Original Research Article
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
8
From page
4939
To page
4946
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
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306690
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