Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P-450 17α)

We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole targetted against 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). Results suggest that the compounds are highly potent inhibitors of the lyase component in comparison to ketoco...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (16), p.4698-4701
Hauptverfasser: Ahmed, Sabbir, Shahid, Imran, Dhanani, Sachin, Owen, Caroline P.
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Sprache:eng
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Zusammenfassung:We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole targetted against 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). Results suggest that the compounds are highly potent inhibitors of the lyase component in comparison to ketoconazole (KTZ). 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 17α-hydroxylase/17,20-lyase (P-450 17α), namely, 17α-hydroxylase (17α-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.06.070