Manetti Dina, Martini Elisabetta, Ghelardini Carla, Dei Silvia, Galeotti Nicoletta, Guandalini Luca, Romanelli Maria Novella, Scapecchi Serena, Teodori Elisabetta, Bartolini Alessandro, Gualtieri Fulvio
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, I-50121, Firenze, Italy.
Bioorg Med Chem Lett. 2003 Jul 21;13(14):2303-6. doi: 10.1016/s0960-894x(03)00437-2.
Extrusion of one of the nitrogens of the piperazine ring of potent nootropic drugs previously described gave 4-aminopiperidine analogues that maintained high cognition enhancing activity in the mouse passive avoidance test. One of the new compounds (9, active at 0.01 mg/kg ip) may represent a new lead for the development of cognition enhancers useful to treat the cognitive deficit produced by neurodegenerative pathologies like Alzheimer's disease.
先前所述的强效益智药物哌嗪环中的一个氮原子被挤出后，得到了4-氨基哌啶类似物，这些类似物在小鼠被动回避试验中保持了较高的认知增强活性。其中一种新化合物（9，腹腔注射剂量为0.01 mg/kg时具有活性）可能代表了一种新的先导化合物，可用于开发有助于治疗由阿尔茨海默病等神经退行性疾病引起的认知缺陷的认知增强剂。
