喹唑啉二酮磺酰胺类：具有口服活性的新型 AMPA 受体竞争性拮抗剂。
Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.
机构信息
Novartis Institutes for BioMedical Research, Global Discovery Chemistry, 4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2011 Jun 1;21(11):3358-61. doi: 10.1016/j.bmcl.2011.04.017. Epub 2011 Apr 8.
PMID:21531559
Abstract
Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models.
摘要
带有磺酰胺基团连接到 N(3)环原子的喹唑啉-2,4-二酮构成了一类新型的竞争性 AMPA 受体拮抗剂。合成的化合物之一 28 具有纳摩尔级的受体亲和力，而该系列的其他例子在动物模型中显示出口服抗惊厥活性。
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