科研之友
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摘要
A series of new 14-hydroxymorphinan analogues with a thiazole or imidazo[2,1-b]thiazole fragment as the heterocyclic function fused to ring C were designed and synthesized. These compounds can be viewed as the result of a direct modification at ring C of the 14-hydroxymorphinan scaffold. Among these compounds, three were identified as having potent binding affinity (similar to 1 nm) at both kappa and mu receptors, and acting as agonists at kappa and partial agonists or antagonists at kappa, receptors. In view of the promising results from studies on compounds with mixed kappa and mu. receptor activities, these new compounds warrant further investigation.
- 出版日期2009-12
- 单位国家新药筛选中心; 中国科学院上海药物研究所
