优化优势结构，以获得选择性和高效的黑色素浓缩素 4 型受体配体。
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10.
PMID:20598533
Abstract
Design, syntheses and structure-activity relationships of N-acetylated piperazine privileged structures containing MC4R agonist compounds were described. The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties.
摘要
描述了含有 MC4R 激动剂化合物的 N-乙酰化哌嗪优势结构的设计、合成和构效关系。最有效的衍生物是低纳摩尔浓度的 MC4R 选择性完全激动剂。该系列中的几种化合物具有中等的药代动力学特性。
Zotero 插件