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强效、选择性的促黑素细胞激素-1（MCH-1）受体拮抗剂。

Potent, selective MCH-1 receptor antagonists.

作者信息

Erickson Shawn D, Banner Bruce, Berthel Steven, Conde-Knape Karin, Falcioni Fiorenza, Hakimi Irina, Hennessy Bernard, Kester Robert F, Kim Kyungjin, Ma Chun, McComas Warren, Mennona Francis, Mischke Steven, Orzechowski Lucy, Qian Yimin, Salari Hamid, Tengi John, Thakkar Kshitij, Taub Rebecca, Tilley Jefferson W, Wang Hong

机构信息

Discovery Chemistry, Hoffmann-La Roche, Inc., 340 Kingsland Street, Nutley, NJ 07110, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1402-6. doi: 10.1016/j.bmcl.2008.01.010. Epub 2008 Jan 8.

DOI:10.1016/j.bmcl.2008.01.010
PMID:18243691
Abstract

This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies and safety.

摘要

本文描述了一系列新型强效、选择性、口服生物可利用且能穿透血脑屏障的MCH-1受体拮抗剂的先导化合物优化过程。该工作的一个主要重点是获得适合体内药效学研究和安全性的选择性特征。

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