Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)).
We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole which has been targetted against the two components of 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)), namely, 17alpha-hydroxylase (17alpha-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are highly potent inhibitors possessing excellent selectivity towards the lyase component.
Ahmed
Sabbir
S
School of Science, University of the West of Scotland, Paisley, PA1 2BE Scotland, UK. sabbir.ahmed@uws.ac.uk
Shahid
Imran
I
Dhanani
Sachin
S
Owen
Caroline P
CP
D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007654:Ketoconazole / Q000494:pharmacology; D008297:Male; D051381:Rats; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013450:Sulfones / Q000737:chemistry; D013737:Testis / Q000201:enzymology*
D004791:Enzyme Inhibitors; D007093:Imidazoles; D013450:Sulfones; D013254:Steroid 17-alpha-Hydroxylase; D007654:Ketoconazole