nNOS-CAPON偶联抑制剂的合成及抗焦虑研究  

Synthesis and Anxiolytic Study of nNOS-CAPON Coupling Inhibitor

作　　者：顾莉洁[1] GU Li-jie(Department of Pharmaceuticl Engineering,Xuzhou Pharmaceutical Vocational School of Jiangsu Province,Xuzhou 221116,China)

机构地区：[1]江苏省徐州医药高等职业学校制药工程系,江苏徐州221116

出　　处：《化学试剂》2024年第10期99-104,共6页Chemical Reagents

摘　　要：合成nNOS-CAPON偶联抑制剂并评价其抗焦虑作用。根据nNOS-CPAON蛋白结构域配体结合部位的结构特点设计并合成了一系列缬氨酸类化合物,通过评价化合物抑制nNOS-CAPON蛋白相互作用(PPI)的活性来筛选化合物,并通过高架十字迷宫实验验证其抗焦虑作用。设计并合成了两个系列共15个化合物,其中N-8具有较好的PPI抑制作用,且在高架十字迷宫实验中显著增加小鼠在开臂的停留时间,具有较强的抗焦虑作用。研究丰富了nNOS-CAPON偶联抑制剂的结构类型,并验证了该类型化合物的抗焦虑作用。A series of valine compounds was designed and synthesized based on the structural features of the ligand binding site of nNOS-CPAON protein.These compounds were screened by evaluating their inhibitory activity against NOS-CAPON protein-protein interaction,and their anti-anxiety effects were verified by an elevated cross maze.The results showed among the fifteen compounds,the N-8 compound exhibited significant inhibition of PPI and markedly increased the time mice spent in the Open Arm of the Elevated Plus Mity of nNOS-CAPON coupling inhibitors,thereby verifying the anxiolytic effects of this class of compounds.

关 键 词：nNOS-CAPON偶联抑制剂 抗焦虑 缬氨酸类化合物 PPI抑制作用 高架十字迷宫实验 

分 类 号：R914[医药卫生—药物化学]