Abstract
A series of pantolactam based compounds were identified as potent antagonists for the androgen receptor (AR). Those that possessed properties suitable for topical delivery were evaluated in the validated Hamster Ear Model. Several compounds were found to be efficacious in reducing wax esters, a major component of sebum, initiating further preclinical work on these compounds.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Topical
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Androgen Receptor Antagonists / chemical synthesis
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Androgen Receptor Antagonists / chemistry
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Androgen Receptor Antagonists / pharmacology*
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Animals
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Cricetinae
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Esters / chemistry
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Esters / metabolism*
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Lactams / chemical synthesis
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Lactams / chemistry
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Lactams / pharmacology*
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Models, Animal
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Models, Molecular
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Molecular Structure
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Receptors, Androgen / metabolism
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Sebum / drug effects*
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Sebum / metabolism
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Stereoisomerism
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Structure-Activity Relationship
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Waxes / chemistry
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Waxes / metabolism*
Substances
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Androgen Receptor Antagonists
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Esters
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Lactams
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Receptors, Androgen
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Waxes