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

Autor:	Katy Bridgwood, Catherine R. Kostlan, Matthew Carroll, Danielle Dettling, Veerabahu Shanmugasundaram, Neil Raheja, Kimberly Jane Wade, Stephen Douglas Barrett, Victor Fedij, David Pocalyko, Smith Yvonne Dorothy, Stephen Fakhoury, Daniel Du, Karen Elaine Sexton, Lain-Yen Hu
Rok vydání:	2011
Předmět:	Models Molecular Lactams Administration Topical Clinical Biochemistry Sebum production Pharmaceutical Science Hamster Pharmacology Crystallography X-Ray Biochemistry Structure-Activity Relationship Cricetinae Drug Discovery Androgen Receptor Antagonists Animals Molecular Biology Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Antagonist Esters Stereoisomerism Sebum Androgen receptor Receptors Androgen Waxes Models Animal Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:5230-5233
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bbeb5016bf2dfd0de38a5184082ceb6 https://doi.org/10.1016/j.bmcl.2011.07.048 Zobrazit plný text záznamu Full Text from ScienceDirect