与布他拉莫有关的抗精神病药物。氯取代基对芳香环影响的研究。
Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings.
作者信息
Humber L G, Sideridis N, Asselin A A, Bruderlein F T, Voith K
出版信息
J Med Chem. 1978 Dec;21(12):1225-31. doi: 10.1021/jm00210a011.
The synthesis of analogues of the antipsychotic drug butaclamol bearing chloro substituents on the benzene rings is described. On the basis of a perceived topographical similarity of a putative chlorophenylethylamine pharmacophore present in these analogues and in VUFB-10032 and doclothepin, agents related to octoclothepin which do not induce catalepsy, they have been tested for "noncataleptic" neuroleptic activity. None of the butaclamol analogues exhibit this type of activity. Depending on the position of the chlorine, the analogues either retained butaclamol-like activity or were inactive.
本文描述了在苯环上带有氯取代基的抗精神病药物布他拉莫类似物的合成。基于这些类似物以及VUFB - 10032和多氯氮平中存在的假定氯苯乙胺药效团在拓扑结构上的相似性，对与不引起僵住症的八氯氮平相关的药物进行了“非僵住症性”抗精神病活性测试。布他拉莫的类似物均未表现出这种类型的活性。根据氯的位置，这些类似物要么保留了布他拉莫样活性，要么无活性。
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