Synthesis of eudistomin D analogues and its effects on adenosine receptors

本文合成了两个从海洋被囊动物橄榄Eudistoma olivaceum中提取的β-咔啉生物碱--eudistomin D的类似物，并研究了它们对腺苷受体亚型A_1、A_2和A_3的亲和力和选择性<2A><3>。两种化合物对A_3受体均表现出中等亲和力。另一方面，合成了咖啡因和eudistomin D的尿嘧啶环上的四个双-N-正丙基类似物，并研究了它们对腺苷受体A_1、A_3和A_1的亲和力和选择性<2A>。其中一个化合物对腺苷受体A_3亚型的亲和力最强。

Two analogues of eudistomin D, a β-carboline alkaloid from a marine tunicate Eudistoma olivaceum, were synthesized, and their affinity and selectivity for adenosine receptor subtypes A_1, A_<2A>, and A_<3> were examined. Both compounds exhibited the moderate affinity to the receptor A_3. On the other hand, four bis-N-n-propyl analogues in the uracil ring of two hybridmolecules of caffeine and eudistomin D were synthesized, and their affinity and selectivity for adenosinereceptors A1, A_<2A>, and A_3 were examined. One of the compounds showed the most potent affinity foradenosine receptor A_3 subtype.