affinity CB2 agonists (5, 16). Substitution at the N1-indole position was then examined. A series of aminoalkylindoles was prepared and several substituted aminoethyl derivatives were active (23−27, 5) at the CB2 receptor. A study of N1 nonaromatic side chain variants provided potent agonists at the CB2 receptor (16, 35−41, 44−47, 49−54, and 57−58). Several polar side chains (alcohols, oxazolidinone) were
已经制备了几种对CB 2
大麻素受体具有高亲和力并且对CB 1受体具有选择性的3-酰基环
吲哚。各种3-酰基取代基进行了调查,和四甲基环组被发现导致高亲和力CB 2激动剂(5,16)。然后检查在N1-
吲哚位置的取代。(A系列aminoalkylindoles的制备和几个取代
氨基乙基衍
生物是活性23 - 27,5在CB)2受体。N1非芳香族侧链变异体的研究为CB 2受体提供了有效的激动剂(16,35 - 41,44 - 47,49 - 54,和57 - 58)。几个极性侧链(
醇类,
恶唑烷酮)的良好的耐受性为CB 2受体的活性(41,50),而其他(酰胺,酸)导致较弱的或无活性的化合物(55和56)。N1芳香族侧链还提供几个高亲和力CB 2受体激动剂(61,63,65,和69),但是在体外CB一般不太有效的2个功能测定法均高于非芳香族侧链类似物。