Author: Mason Peter Greer Valerie P. Kirby Andrew J. Simons Claire Nicholls Paul J. Smith H. John
Publisher: Informa Healthcare
ISSN: 1475-6366
Source: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.18, Iss.6, 2003-12, pp. : 511-528
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Abstract
Some aryl substituted methyl 2-(4-nitrophenyl)-4-oxo-4-phenylbutanoates generally had poor to moderate inhibitory potency (4-73%) towards rat liver microsomal retinoic acid metabolising enzymes compared with ketoconazole (80%). Conversion to the corresponding 3-(4-nitrophenyl)-1-aryl-1,4-butanediols considerably increased potency (29-78%). The 4-iodophenyl analogue, (30) and the 4-iodo- (45) and 4-methoxyphenyl (46) analogues, were the most potent in both series respectively. The corresponding 5-membered lactones, in the three instances examined, were also potent (52%, 67%, 69%) as were the
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