Mazzone G, Pignatello R, Panico A, Mazzone S, Puglisi G, Pennisi G, Raciti G, Mazzone P, Matera M
Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Catania, Italy.
Pharmazie. 1992 Dec;47(12):902-10.
Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine and clonidine and L-amfetamine-induced hypermotility) and in vitro tests, to assay their effect on rat brain mitochondria by a kinuramine fluorimetric assay. In vivo, all the tested compounds significatively influenced the evaluative parameters used. As regards in vitro test, all compounds displayed MAOI activity at a concentration of 1.10(-4) mol.l-1, which was significant in several cases. In the discussion of the results, the influence of the structure on the biological activity of the prepared compounds was delineated.
合成了三组2-噻唑基肼，并通过体内试验评估其单胺氧化酶抑制（MAOI）活性，以测定它们对几个与MAOI活性相关参数的影响（酪胺和可乐定引起的血压变化以及左旋苯丙胺引起的运动亢进），还通过体外试验，采用喹哪明荧光分析法测定它们对大鼠脑线粒体的影响。在体内，所有受试化合物均对所使用的评估参数有显著影响。至于体外试验，所有化合物在浓度为1.10（-4）mol·l-1时均显示出MAOI活性，在几种情况下这一活性具有显著性。在结果讨论中，阐述了结构对所制备化合物生物活性的影响。
