Bernardi L
Arzneimittelforschung. 1979;29(8a):1204-6.
The author reports the rationale of a line of research that has led to pharmacologically active ergoline derivatives from the more complex ergot alkaloids. Specific compounds showing oxytocic, alpha-adrenolytic and antiserotoninic activity were synthesized and the relationship between structure and activity discussed. Out of the compounds, 10-methoxy-1,6-dimethyl-ergoline-8 beta-methanol-(5-bromonicotinate) (nicergoline) was chosen as the most interesting product for a detailed further development.
作者报告了一系列研究的基本原理,这些研究已从更复杂的麦角生物碱中获得了具有药理活性的麦角灵衍生物。合成了具有催产、α-肾上腺素能阻断和抗血清素活性的特定化合物,并讨论了结构与活性之间的关系。在这些化合物中,10-甲氧基-1,6-二甲基-麦角灵-8β-甲醇-(5-溴烟酸酯)(尼麦角林)被选为最具吸引力的产品,以便进行详细的进一步开发。