双位点芳基哌嗪-六氢吡嗪并喹啉化合物的设计、合成与生物评价作为优先多巴胺 D3 受体配体。
Design, synthesis and biological evaluation of bitopic arylpiperazine-hexahydro-pyrazinoquinolines as preferential dopamine D3 receptor ligands.
机构信息
School of Chemistry and Chemical Engineering, Institute of Pharmaceutical Engineering, Southeast University, 87 Dingjiaqiao, Nanjing, Jiangsu 210096, PR China; School of Chemistry and Chemical Engineering, Yancheng Institute of Technology, 211 Jianjun East Road, Yancheng, Jiangsu 224051, PR China.
School of Chemistry and Chemical Engineering, Institute of Pharmaceutical Engineering, Southeast University, 87 Dingjiaqiao, Nanjing, Jiangsu 210096, PR China.
出版信息
Bioorg Chem. 2018 Apr;77:125-135. doi: 10.1016/j.bioorg.2017.12.026. Epub 2018 Jan 9.
Three series of bitobic arylpiperazine-phenyl-hexahydropyrazinoquino- lines analogues were designed, synthesizedand evaluated as a novel class of selective ligands for the dopamine D3 receptor. Compounds 15a (K of 11.7 ± 1.8 and 373 nM at D3 and D2, respectively), 15c (K of 5.49 and 264 nM at D3 and D2, respectively), 15e (K of 14.9 and 325 nM at D3 and D2, respectively), 15i (K of 13.8 and 401 nM at D3 and D2, respectively) and 15l (K of 13.6 and 870 nM at D3 and D2, respectively) were found to demonstrate good binding affinity and selectivity, and especially compound 15c showeda similar binding affinity and selectivity compared with the contrast drug BP897.
设计、合成并评价了三系列双苯哌嗪-苯基-六氢吡嗪喹啉类似物，作为多巴胺 D3 受体的新型选择性配体。化合物 15a（D3 和 D2 受体的 K i 值分别为 11.7±1.8 和 373nM）、15c（D3 和 D2 受体的 K i 值分别为 5.49 和 264nM）、15e（D3 和 D2 受体的 K i 值分别为 14.9 和 325nM）、15i（D3 和 D2 受体的 K i 值分别为 13.8 和 401nM）和 15l（D3 和 D2 受体的 K i 值分别为 13.6 和 870nM）表现出良好的结合亲和力和选择性，特别是化合物 15c 与对照药物 BP897 相比具有相似的结合亲和力和选择性。
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