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Bioorg Med Chem Lett. 2010 Jan 15;20(2):726-9. doi: 10.1016/j.bmcl.2009.11.070. Epub 2009 Dec 11.

Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists.

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Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan.


This Letter describes the synthesis and evaluation of mGluR7 antagonists in the isoxazolopyridone series. In the course of modification in this class, novel solid support synthesis of the isoxazolopyridone scaffold was developed. Subsequent chemical modification 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.

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