Dann O, Steuding W, Lisson K G, Seidel H R, Fink E, Nickel P
Arzneimittelforschung. 1982;32(10):1219-23.
Antimalarial 6-aminoquinolines (1a-c) were acylated (3a-c, 5a) and alkylated (4a-c, 6a) at the secondary aromatic 6-amino group with the aim of studying the influence of a tertiary aromatic 6-amino group on antimalarial activity and toxicity. 4 derivatives (9e-g) of 4-amino-7-chloroquinoline with a tertiary aromatic 4-amino group were synthesized to study the influence of such a variation on the biological activity of the 4-aminoquinolines. The N-alkylated derivatives 4a-c, 6a, 9f-g were active against malaria (P. vinckei/mice).
为了研究叔芳基 6-氨基对抗疟活性和毒性的影响，对抗疟 6-氨基喹啉（1a - c）的仲芳基 6-氨基进行了酰化（3a - c，5a）和烷基化（4a - c，6a）。合成了具有叔芳基 4-氨基的 4-氨基-7-氯喹啉的 4 种衍生物（9e - g），以研究这种变化对 4-氨基喹啉生物活性的影响。N-烷基化衍生物 4a - c、6a、9f - g 对疟疾（文氏疟原虫/小鼠）具有活性。
