The role of fluorine substitution in the structure-activity relationships (SAR) of classical cannabinoids.
The role of fluorine substitution in the structure-activity relationships (SAR) of classical cannabinoids.
复制标题
氟取代在经典大麻素结构活性关系（SAR）中的作用。
DOI：
10.1016/j.bmcl.2007.01.006
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发表时间：
2007
影响因子：
2.7
通讯作者：
Razdan,RajK
中科院分区：
文献类型：
--
作者：
Crocker,PeterJ;Mahadevan,Anu;Wiley,JennyL;Martin,BillyR;Razdan,RajK
A facile synthesis of 1-fluoro-1-deoxy-Δ8-THC analogs with side chains seven carbons in length, in the alkane/ene/yne- series (6, 5, and 4), was achieved from 1-fluoro-3,5-dimethoxybenzene (1). In vitro studies show that substitution by a fluorine has a significant detrimental effect on CB1 binding which is supported by in vivo testing. The implications of these results on the SAR of classical cannabinoids are discussed.
