title: Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.
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.
authors.affiliation: Department of Medicinal Chemistry, Michigan Laboratories, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. karen.sexton@hotmail.co.uk
authors.forename: Karen E
authors.initials: KE
authors.lastname: Sexton
authors.forename: Stephen
authors.initials: S
authors.lastname: Barrett
authors.forename: Katy
authors.initials: K
authors.lastname: Bridgwood
authors.forename: Matthew
authors.initials: M
authors.lastname: Carroll
authors.forename: Danielle
authors.initials: D
authors.lastname: Dettling
authors.forename: Daniel
authors.initials: D
authors.lastname: Du
authors.forename: Stephen
authors.initials: S
authors.lastname: Fakhoury
authors.forename: Victor
authors.initials: V
authors.lastname: Fedij
authors.forename: Lain-Yen
authors.initials: LY
authors.lastname: Hu
authors.forename: Catherine
authors.initials: C
authors.lastname: Kostlan
authors.forename: David
authors.initials: D
authors.lastname: Pocalyko
authors.forename: Neil
authors.initials: N
authors.lastname: Raheja
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Smith
authors.forename: Veerabahu
authors.initials: V
authors.lastname: Shanmugasundaram
authors.forename: Kimberly
authors.initials: K
authors.lastname: Wade
mesh_terms: D000287:Administration, Topical; D059002:Androgen Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D006224:Cricetinae; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004952:Esters / Q000737:chemistry / Q000378:metabolism*; D007769:Lactams / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D023421:Models, Animal; D008958:Models, Molecular; D015394:Molecular Structure; D011944:Receptors, Androgen / Q000378:metabolism; D012629:Sebum / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014885:Waxes / Q000737:chemistry / Q000378:metabolism*
chemical_list: D059002:Androgen Receptor Antagonists; D004952:Esters; D007769:Lactams; D011944:Receptors, Androgen; D014885:Waxes