Flaugh M E, Mullen D L, Fuller R W, Mason N R
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
J Med Chem. 1988 Sep;31(9):1746-53. doi: 10.1021/jm00117a013.
A series of 6-substituted tricyclic ergoline partial structures has been synthesized and found to possess very strong serotonin agonist activity. A methoxy group at the 6-position greatly enhances activity, but at the expense of compound stability. Substituting the 6-position with protophyllic groups that are also electron-withdrawing in character enhances both activity and stability.
已经合成了一系列6-取代的三环麦角灵部分结构，并发现它们具有非常强的血清素激动剂活性。6位上的甲氧基极大地增强了活性，但以化合物稳定性为代价。用同样具有吸电子特性的原叶基取代6位，可同时提高活性和稳定性。
