Nawrocka W, Liszkiewicz H, Wilimowski M, Rutkowska M, Barczyńska J, Kedzierska-Goździk L, Wojewódzki W, Szelag A
Department of Technology of Drugs, School of Medicine, Wrocław, Poland.
Acta Pol Pharm. 1994;51(3):243-8.
2-Thioxo-1H-2,3,4,5-tetrahydropyrido[2,3-e]-1,3,4-triazep in -5-ones [I] and 2-thioxo-1H-2,3,4,-5-tetrahydro-1,3,4-benzotriazepin-5-ones [V] furnish with methyl, ethyl and phenyl chloroformates two series of the corresponding 3-methoxy-, ethoxy- and phenoxycarbonyl triazepines. In the pharmacological screening, compounds [I], [V] and [II] showed an antianxiety activity in the four plate test, compounds [II] and [III] inhibited the 5-HTP- induced head twitches, and compound [VI] showed an analgesic activity in the "writing" test. The replacement of the benzene ring by the pyridine one in triazepines is accompanied by the enhancement of anxiolytic activity as well as toxicity.
2-硫代-1H-2,3,4,5-四氢吡啶并[2,3-e]-1,3,4-三氮杂卓-5-酮[I]和2-硫代-1H-2,3,4,5-四氢-1,3,4-苯并三氮杂卓-5-酮[V]与氯甲酸甲酯、乙酯和苯酯反应,生成了两个系列相应的3-甲氧基、乙氧基和苯氧基羰基三氮杂卓。在药理筛选中,化合物[I]、[V]和[II]在四板试验中显示出抗焦虑活性,化合物[II]和[III]抑制5-羟色氨酸诱导的头部抽搐,化合物[VI]在“书写”试验中显示出镇痛活性。三氮杂卓中吡啶环取代苯环会伴随着抗焦虑活性以及毒性的增强。