Bringmann G, Hoerr V, Holzgrabe U, Stich A
Institut für Organische Chemie, Dept. of Tropical Medicine and Epidemic Control, Würzburg, Germany.
Pharmazie. 2003 May;58(5):343-6.
In view of the need to develop new drugs against human African trypanosomiasis, a series of naturally occurring naphthylisoquinoline alkaloids, axially chiral acetogenic products derived from tropical plants, have been investigated for their activity against Trypanosoma brucei brucei TC 221. Likewise compounds corresponding to the two molecular portions, the naphthalene and the isoquinoline parts were tested, as well as molecules related to the central biaryl core of the alkaloids. Among all compounds tested, the natural, genuine alkaloids themselves, in particular dioncophylline B with its biaryl system and a moderate number of free hydroxy functions, showed the highest activities. Our results demonstrate that naphthylisoquinoline alkaloids constitute an interesting novel class of antitrypanosomal compounds worth further optimization.
鉴于开发治疗人类非洲锥虫病新药的需求，一系列天然存在的萘基异喹啉生物碱，即源自热带植物的轴向手性产乙酸产物，已针对其对布氏布氏锥虫TC 221的活性进行了研究。同样，对与两个分子部分（萘和异喹啉部分）相对应的化合物以及与生物碱中心联芳基核心相关的分子进行了测试。在所有测试的化合物中，天然的、纯正的生物碱本身，特别是具有联芳基系统和适量游离羟基官能团的二酮叶啉B，表现出最高的活性。我们的结果表明，萘基异喹啉生物碱构成了一类有趣的新型抗锥虫化合物，值得进一步优化。
