Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists

被引：27

作者：

Nakamura, Masayuki ^{[1
]}

Kurihara, Hideki ^{[1
]}

Suzuki, Gentaroh ^{[1
]}

Mitsuya, Morihiro ^{[1
]}

Ohkubo, Mitsuru ^{[1
]}

Ohta, Hisashi ^{[1
]}

机构：

[1] Banyu Pharmaceut Co Ltd, Banyu Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 02期

关键词：

mGluR7; Antagonist; Solid support synthesis; Isoxazolopyridone; WORKING-MEMORY; LOCALIZATION; MGLUR7; PROTEIN; RAT;

D O I：

10.1016/j.bmcl.2009.11.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This Letter describes the synthesis and evaluation of mGluR7 antagonists in the isoxazolopyridone series. In the course of modi. cation in this class, novel solid support synthesis of the isoxazolopyridone scaffold was developed. Subsequent chemical modi. cation led to the identification of several potent derivatives with improved physicochemical properties compared to a hit compound 1. Among these, 2 showed good oral bioavailability and brain penetrability, suggesting that 2 may be useful for in vivo study to elucidate the role of mGluR7. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：726 / 729

页数：4

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