Avramova P D, Danchev N D, Buyukliev R T
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sofia, Bulgaria.
Pharmazie. 1999 Jun;54(6):409-11.
The synthesis, pharmacology and toxicology of four morpholine derivatives from 1-(2-arylmorpholino)-3-phenyl-3-propanonoxime and the synthesis of two anilides are described. The structures of the synthesized derivatives were proved by IR, 1H NMR and occasionally with 13C NMR. The acute toxicity of the compounds in mice was determined. A comparative pharmacological study of the in vivo effect on the central nervous system was realised by the following screening tests: pentobarbital induced sleeping time, locomotor activity and behaviour despair test for antidepressive activity. The most active compound was 1-(2-phenylmorpholino)-3-phenyl-3-propanonoxime (2b) which showed low toxicity and antidepressive activity at a dose of 1/10 LD50.
描述了由1-(2-芳基吗啉基)-3-苯基-3-丙肟制得的四种吗啉衍生物的合成、药理学和毒理学以及两种酰苯胺的合成。通过红外光谱、1H核磁共振光谱，偶尔也用13C核磁共振光谱对合成衍生物的结构进行了确证。测定了这些化合物对小鼠的急性毒性。通过以下筛选试验对其对中枢神经系统的体内作用进行了比较药理学研究：戊巴比妥诱导睡眠时间、自发活动以及行为绝望试验以检测抗抑郁活性。活性最高的化合物是1-(2-苯基吗啉基)-3-苯基-3-丙肟(2b)，其在1/10半数致死剂量时表现出低毒性和抗抑郁活性。
