Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity
作者:Manuel Koller、Kurt Lingenhoehl、Markus Schmutz、Ivan-Toma Vranesic、Joerg Kallen、Yves P. Auberson、David A. Carcache、Henri Mattes、Silvio Ofner、David Orain、Stephan Urwyler
DOI:10.1016/j.bmcl.2011.04.017
日期:2011.6
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.
带有与N(3)环原子相连的磺酰胺基的喹唑啉2,4-二酮构成一类新的竞争性AMPA受体拮抗剂。一种合成的化合物28显示出纳摩尔受体亲和力,而该系列的其他实例在动物模型中显示出口服抗惊厥活性。