Department of Chemistry, University of Hawaii at Manoa, Honolulu, Hawaii 96822, USA.
J Med Chem. 2010 Aug 12;53(15):5656-66. doi: 10.1021/jm100390h.
The aliphatic side chain plays a pivotal role in determining the cannabinergic potency of tricyclic classical cannabinoids. We have synthesized a series of analogues in which the C3 position is substituted either directly or through a one-carbon atom linker with an adamantylamine or with an oxa- or an oxazaadamantane. The oxaadamantane pharmacophore in analogue 16 showed the best binding profile for both receptors.
脂肪族侧链在确定三环经典大麻素的大麻素效力方面起着关键作用。我们已经合成了一系列类似物,其中 C3 位置直接或以一个碳原子连接体与金刚烷胺或氧代或氮杂金刚烷取代。类似物 16 中的氧代金刚烷药效团对两个受体都显示出最佳的结合谱。