Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy.
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1936-9. doi: 10.1016/j.bmcl.2012.01.045. Epub 2012 Jan 25.
A series of analogs of DM235 and MN19, characterized by rings with different size, have been prepared and evaluated for their nootropic activity in the mouse passive-avoidance test. It was found that the optimal ring size for the analogs of DM235, showing endocyclic both amidic groups, is 6 or 7 atoms. For the compounds structurally related to MN19, carrying an exocyclic amide group, the piperidine ring is the moiety which gives the most interesting compounds.
一系列 DM235 和 MN19 的类似物已被制备,其特点是具有不同大小的环,并在小鼠被动回避试验中评估其益智活性。结果发现,对于显示内酰胺基的 DM235 类似物,最佳环大小为 6 或 7 个原子。对于与 MN19 结构相关的化合物,携带一个外酰胺基团,哌啶环是赋予最有趣化合物的部分。