Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids

V C Njar; I P Nnane; A M Brodie

doi:10.1016/s0960-894x(00)00391-7

Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1905-8. doi: 10.1016/s0960-894x(00)00391-7.

Authors

V C Njar¹, I P Nnane, A M Brodie

Affiliation

¹ Department of Pharmacology and Experimental Therapeutics, School of Medicine, University of Maryland, Baltimore 21021-1559, USA. vnjar001@umaryland.edu

PMID: 10987414
DOI: 10.1016/s0960-894x(00)00391-7

Abstract

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.

MeSH terms

Animals
Azoles / pharmacology*
Cricetinae
Cytochrome P-450 Enzyme Inhibitors*
Cytochrome P-450 Enzyme System
Enzyme Inhibitors / pharmacology*
Retinoic Acid 4-Hydroxylase
Retinoids / pharmacology*
Tretinoin / metabolism

Substances

Azoles
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors
Retinoids
Tretinoin
Cytochrome P-450 Enzyme System
Retinoic Acid 4-Hydroxylase