从吡啶酮到咪唑并[1,2-a]吡啶的支架跃迁。代谢型谷氨酸 2 受体的新型正变构调节剂。
Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.
机构信息
Research Informatics, Johnson & Johnson, Pharmaceutical Research & Development, Janssen-Cilag S.A., Calle Jarama 75, Poligono Industrial, Toledo 45007, Spain.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10.
PMID:19932615
Abstract
Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies.
摘要
通过形状和静电相似性，确定咪唑并[1,2-a]吡啶类化合物为代谢型谷氨酸 2 受体的新型正变构调节剂。随后对其进行了合成和 SAR 描述。发现了具有高活性、选择性和代谢稳定性的化合物，为进一步的研究提供了有前景的途径。
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