舒缓激肽拮抗剂Martinellic 酸的全合成研究

Martinellic acid was isolated from the tropical plant Martinella Iquitosensis, which had been shown to possess antagonistic behavior towards bradykinin receptors. In order to study the structure and activity relationship, we explored the intermolecular azo[2+4] cycloaddition reaction as a general method for the synthesis of the tricyclic core of martinellic acid, It has the potential to be extended into the synthesis of many martinellic acid derivatives.

Martinellic acid是从热带植物Martinella iquitosensis分离得到的具有吡咯并[3, 2-c]喹啉骨架类型的天然生物碱，它对缓激肽受体有较强的拮抗作用,到目前为止它是发现的第一个对该受体有活性的非肽类天然产物。该生物碱的全合成未见文献报导，因而对其进行全合成研究，并以其为先导化合物合成一系列结构类似的衍生物，进一步研究其构效关系，从中有可能发现新结构类型的抗炎、抗过敏药物.本项研究既具有一定的理论意义，又有重氖导室庖濉