A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.
A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.
复制标题
一种基于烯丙基菌株设计构象限制类似物的方法：合成一类新型的具有丙烯酰胺结构的非竞争性NMDA受体拮抗剂。
DOI：
10.1021/jm030226n
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发表时间：
2003
影响因子：
7.3
通讯作者：
S. Shuto
中科院分区：
文献类型：
--
作者：
Y. Ohmori;A. Yamashita;R. Tsujita;Tamotsu Yamamoto;Kaku Taniuchi;A. Matsuda;S. Shuto
利用烯丙基链的方法设计了一系列弱NMDA受体拮抗剂米那普仑的构象限制性类似物。构象分析研究表明，基于烯丙基应变的构象限制确实发生，并且通过构象限制有效地提高了对NMDA受体的亲和力。
A series of conformationally restricted analogues of milnacipran, a weak NMDA receptor antagonist, were designed by a method based on allylic strain. The conformational analysis study showed that the allylic-strain-based conformational restriction indeed occurred and that the affinity for the NMDA receptor was efficiently improved by the conformational restriction.