发现一系列新型黑色素聚集激素受体 1 拮抗剂，可用于治疗肥胖症。
Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
机构信息
Department of Medicinal Chemistry, Amgen, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7001-5. doi: 10.1016/j.bmcl.2011.09.110. Epub 2011 Oct 5.
PMID:22019296
Abstract
A new class of MCHR1 antagonists was discovered via a high-throughput screen. Optimization of the lead structure resulted in the identification of indole 10e. This compound possesses good pharmacokinetic properties across preclinical species and is efficacious in reducing food consumption in an MCH cannulated rat model and a cynomolgus monkey food consumption model.
摘要
一种新型的 MCHR1 拮抗剂是通过高通量筛选发现的。通过对先导结构的优化，确定了吲哚 10e 为候选化合物。该化合物在临床前动物中具有良好的药代动力学特性，能够有效减少 MCH 灌胃大鼠模型和食蟹猴食物消耗模型中的食物摄入量。
Zotero 插件