G. A. Khodarahmi, H. J. Smith, Paul J. Nicholls
Sep 1, 1998
Citations
0
Influential Citations
7
Citations
Journal
Journal of Pharmacy and Pharmacology
Abstract
The low stereospecificity of the enantiomers of 1-[(benzofuran-2-yl)-4-chlorophenyl-methyl]imidazole (6, R=H, R'=4'-Cl) and the corresponding 4-fluoro compound as inhibitors of aromatase (P450 Arom ) has been explored using 1-(5,7-dichlorobenzofuran-2-yl)-1-(1H-imidaz-1-yl)ethane (7, R 1 =R 2 =Cl, R=CH 3 ), -propane (7, R 1 =R 2 =Cl, R = C 2 H 5 ), and the corresponding 5,7-dibromo compounds resolved as their dibenzoyl-D (or -L) tartrates. Low enantioselectivity ratios of 4.8 (5,7-diCl) and 12.6 (5,7-diBr) were shown for the ethanes. The values for the corresponding propanes were 8.3 and 5.2, respectively, and for these compounds the stereoselectivity was reversed.