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目的设计合成3,4-二氢喹啉-2(1H)-酮类化合物,考察其对D2、5-HT2A、5-HT1A受体的亲和力,并对代表化合物进行体内抗精神分裂活性测试。方法 7-羟基-3,4-二氢喹啉-2(1H)-酮与二卤代烷进行O-烷基化反应,再与相应的哌啶衍生物反应得到目标产物(Ⅰ1~Ⅰ11);对目标化合物进行了D2、5-HT2A、5-HT1A受体亲和力初步试验,并选择化合物Ⅰ7进行体内抗阿朴吗啡诱导的小鼠精神分裂模型实验。结果与结论共合成了11个新化合物,其结构经质谱及核磁共振氢谱确证。其中化合物Ⅰ7体内外活性良好,具有进一步研究的价值。
OBJECTIVE To design and synthesize 3,4-dihydroquinolin-2 (1H) -ones and investigate their affinity to D2,5-HT2A and 5-HT1A receptors and to test their anti-schizophrenic activity in vivo. Method O-Alkylation of 7-hydroxy-3,4-dihydroquinolin-2 (1H) -one with dihalogenoalkane followed by reaction with the corresponding piperidine derivative to obtain the desired product (I1 ~ I11) The target compounds were initially tested for D2,5-HT2A, 5-HT1A receptor affinity and Compound I7 was selected for in vivo anti-apomorphine-induced mouse schizophrenia model experiments. RESULTS AND CONCLUSIONS A total of 11 new compounds were synthesized and their structures were confirmed by MS and 1H-NMR. Among them, the activity of compound Ⅰ7 in vitro and in vivo was good, which has the value of further research.