摘要
利用Hansch方法 ,研究了 37种benztropine类化合物diphenylmethoxy部位苯环取代基结构与其活性的定量关系 .结果表明 :苯环取代基的电性和体积等均是影响该类化合物与多巴胺转运蛋白亲和力的重要因素 .所得到的benztropine类化合物diphenylmethoxy部位取代基的综合结构效应 。
The effect of the aromatic substituents in the diphenylmethoxy of benztropine analogs on the affinity for the dopamine transporter is studied using Hansch method. QSAR is found by stepwise and bachward methods of SPSS program. It is demonstrated that the binding affinity is a function of the following parameters: ∑ σ p (∑R,∑F), R m2 and R m4 . It is shown that both steric factors and electronic components of substituents of diphenylmethoxy are significant as to the binding affinity at the dopamine transporter. The results may be useful in understanding the interaction of dopamine transporter with benztropine analogs and in designing new benztropine ligands as molecular probes for the dopamine transporter.
出处
《北京师范大学学报（自然科学版）》
CAS
CSCD
北大核心
2001年第1期74-78,共5页
Journal of Beijing Normal University(Natural Science)
基金
教育部博士点基金资助项目
北京师范大学青年基金资助项目 !(2 72 0 0 7)
