Toscano L, Grisanti G, Fioriello G, Seghetti E, Bianchetti A, Bossoni G, Riva M
J Med Chem. 1976 Feb;19(2):208-13. doi: 10.1021/jm00224a003.
Basic derivatives of 6,7-dihydroindolo[1,7-ab][1]benzazepine and 6H-indolo[7,1-cd][1,5]benzoxazepine incorporating the imipramine basic side chain were synthesized and screened for antidepressant activity in mice. With few exceptions, the compounds unsubstituted at C-2 antagonized reserpine-induced ptosis and hypothermia showing negligible anticholinergic and antihistaminic properties. The compound 1-[2-(N-methyl-N-benzylamino)ethyl]-6,7-dihydroindolo[1,7-ab][1]benzazepine had the highest toxicity-activity ratio.
合成了包含丙咪嗪碱性侧链的6,7-二氢吲哚并[1,7 - ab][1]苯并氮杂䓬和6H-吲哚并[7,1 - cd][1,5]苯并恶唑嗪的基本衍生物，并在小鼠中筛选其抗抑郁活性。除少数例外，在C-2位未被取代的化合物可拮抗利血平诱导的眼睑下垂和体温过低，显示出可忽略不计的抗胆碱能和抗组胺特性。化合物1-[2-(N-甲基-N-苄基氨基)乙基]-6,7-二氢吲哚并[1,7 - ab][1]苯并氮杂䓬具有最高的毒性-活性比。
