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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 ORCID:, Jones, Glenville and Simons, Claire ORCID: 2010. Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides. Bioorganic & Medicinal Chemistry 18 (14) , pp. 4939-4946. 10.1016/j.bmc.2010.06.011

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords: N-(2-(1H-Imidazol-1-yl)-2-phenylethyl)arylamides ; Benzofuran-2-carboxamides ; CYP24A1 ; Enzyme inhibition ; Molecular modelling
Publisher: Elsevier
ISSN: 0968-0896
Last Modified: 05 Jan 2024 05:58

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