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 |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.06.070 |