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利用Hansch方法,研究了具有2-毗咯烷基侧链的苯酰胺类化合物的苯环取代基结构与其活性的定量关系.结果表明:苯环R3位取代基的脂溶性、电性,R5位取代基的共振效应等均是影响化合物与多巴胺D2受体亲和力的因素.所得到的取代基的综合结构效应对阐明D2受体-配体的相互作用机制及设计新的配体具有指导意义.
The Hansch method was used to study the quantitative relationship between the structure of benzene ring substituents and the activity of benzoylamides with 2-pyrrolidinyl side chains. The results showed that the lipophilicity, electrical property and the resonance effect of the R5 substituent on the R3 substituent of the benzene ring are the factors that affect the affinity of the compound with the dopamine D2 receptor. The overall structural effect of the resulting substituents is instructive in elucidating the D2 receptor-ligand interaction mechanism and in designing novel ligands.