2. Academic Validation
  3. Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides

Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides

  • Bioorg Med Chem. 2010 Jul 15;18(14):4939-46. doi: 10.1016/j.bmc.2010.06.011.
Ahmed S Aboraia 1,  Sook Wah Yee,  Mohamed Sayed Gomaa,  Nikhil Shah,  Anna C Robotham,  Bart Makowski,  David Prosser,  Andrea Brancale,  Glenville Jones,  Claire Simons
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.
PMID: 20594862 DOI: 10.1016/j.bmc.2010.06.011
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 microM compared with the standard ketoconazole IC50 0.52 microM, with the styryl derivative (11c) displaying enhanced activity (IC50=0.3 microM) compared with the standard, providing a useful preliminary lead for drug development.

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