Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids.
Novel (+/-)-4-azolyl retinoic acid analogues 4, 5, 7 and 8 have been designed and synthesized and have been shown to be powerful inhibitors of hamster microsomal all-trans-retinoic acid 4-hydroxylase enzyme(s). (+/-)-4-(1H-Imidazol-1-yl)retinoic acid (4) is the most potent inhibitor of this enzyme reported to date.
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Department of Pharmacology and Experimental Therapeutics, School of Medicine, University of Maryland, Baltimore 21021-1559, USA. vnjar001@umaryland.edu
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D000818:Animals; D001393:Azoles / Q000494:pharmacology*; D006224:Cricetinae; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D000072516:Retinoic Acid 4-Hydroxylase; D012176:Retinoids / Q000494:pharmacology*; D014212:Tretinoin / Q000378:metabolism
D001393:Azoles; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D012176:Retinoids; D014212:Tretinoin; D003577:Cytochrome P-450 Enzyme System; D000072516:Retinoic Acid 4-Hydroxylase