作为雄激素受体拮抗剂的泛酰巯基乙胺用于局部皮脂抑制。
Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.
机构信息
Department of Medicinal Chemistry, Michigan Laboratories, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5230-3. doi: 10.1016/j.bmcl.2011.07.048. Epub 2011 Jul 23.
PMID:21831636
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.
摘要
一系列的泛酰巯基乙胺类化合物被鉴定为有效的雄激素受体（AR）拮抗剂。那些具有适合局部递药特性的化合物在已验证的仓鼠耳部模型中进行了评估。一些化合物被发现能有效减少皮脂的主要成分——蜡酯，这促使对这些化合物进行进一步的临床前研究。
Zotero 插件