Giannotti D, Viti G, Sbraci P, Pestellini V, Volterra G, Borsini F, Lecci A, Meli A, Dapporto P, Paoli P
Dipartimento Ricerche Chimiche e Farmacologiche, A. Menarini Industrie Farmaceutiche Riunite S.r.l., Firenze, Italy.
J Med Chem. 1991 Apr;34(4):1356-62. doi: 10.1021/jm00108a018.
A new series of 11-[(aminoalkyl)carbonyl] derivatives of 6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide (10-39) were synthesized and evaluated for potential antidepressant activity in the apomorphine-induced hypothermia (Apo 16) test. Effects on reserpine-induced hypothermia and toxicity for the most potent antagonists of Apo 16 hypothermia were also studied. Structure-activity relationships are reported. Anticholinergic effects were evaluated for compound 12, identified as the most potent and least toxic in this series, by assessing physostigmine lethality. Compound 12 was also subjected to X-ray analysis.
合成了一系列新的6,11-二氢二苯并[c,f][1,2,5]噻二氮杂卓5,5-二氧化物（10-39）的11-[(氨基烷基)羰基]衍生物，并在阿扑吗啡诱导的体温过低（Apo 16）试验中评估其潜在的抗抑郁活性。还研究了它们对利血平诱导的体温过低的影响以及对Apo 16体温过低最有效的拮抗剂的毒性。报告了构效关系。通过评估毒扁豆碱致死率，对该系列中最有效且毒性最小的化合物12进行了抗胆碱能作用评估。化合物12也进行了X射线分析。
