Pantolactams as androgen receptor antagonists for the topical suppression of sebum production

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 majo...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-09, Vol.21 (18), p.5230-5233
Hauptverfasser:	Sexton, Karen E., Barrett, Stephen, Bridgwood, Katy, Carroll, Matthew, Dettling, Danielle, Du, Daniel, Fakhoury, Stephen, Fedij, Victor, Hu, Lain-Yen, Kostlan, Catherine, Pocalyko, David, Raheja, Neil, Smith, Yvonne, Shanmugasundaram, Veerabahu, Wade, Kimberly
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Topical Androgen receptor Androgen Receptor Antagonists - chemical synthesis Androgen Receptor Antagonists - chemistry Androgen Receptor Antagonists - pharmacology androgen receptors Animals Antagonist antagonists Biological and medical sciences chemistry Cricetinae Crystallography, X-Ray Dose-Response Relationship, Drug Esters - chemistry Esters - metabolism hamsters Lactams - chemical synthesis Lactams - chemistry Lactams - pharmacology Medical sciences Models, Animal Models, Molecular Molecular Structure Pharmacology. Drug treatments Receptors, Androgen - metabolism Sebum Sebum - drug effects Sebum - metabolism Skin, nail, hair, dermoskeleton Stereoisomerism Structure-Activity Relationship Topical wax esters Waxes - chemistry Waxes - metabolism
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.07.048