Schulze W, Letsch G, Gutsche W, Wohlrabe K, Tresselt D
Pharmazie. 1984 May;39(5):320-2.
Tilorone (free base) reacts with alkyl halides forming quaternary ammonium salts. Bis- as well as mono quaternary compounds (2 resp. 3) were synthesized. The tilorone-bis-methoiodide (2a) was converted to several carbonyl derivatives (4 and 5). All produced compounds did not show any cytostatic activity against the murine leukemias L 1210 and P 388 in vivo. Especially the bis-quaternary derivatives 2 were highly toxic in the mouse.
替洛隆(游离碱)与卤代烷反应生成季铵盐。合成了双季铵化合物和单季铵化合物(分别为2和3)。替洛隆双甲碘化物(2a)被转化为几种羰基衍生物(4和5)。所有生成的化合物在体内对小鼠白血病L 1210和P 388均未显示出任何细胞抑制活性。特别是双季铵衍生物2对小鼠具有高毒性。