Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

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 and Simons, Claire 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

Full text not available from this repository.

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.

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: 02 Jun 2019 22:51
URI: http://orca-mwe.cf.ac.uk/id/eprint/7468

Citation Data

Cited 11 times in Google Scholar. View in Google Scholar

Cited 15 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item