Novel Multipotent Tacrine-Dihydropyridine Hybrids with Improved Acetylcholinesterase Inhibitory and Neuroprotective Activities as Potential Drugs for the Treatment of Alzheimer's Disease

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• 作者：José ; Marco-Contelles ; Rafael Le&oacute ; n ; Crist&oacute ; bal de los Rí ; os ; Antonio Guglietta ; José ; Terencio ; Manuela G. L&oacute ; pez ; Antonio G. Garcí ; a ; Mercedes Villarroya
• 刊名：Journal of Medicinal Chemistry
• 出版年：2006
• 出版时间：December 28, 2006
• 年：2006
• 卷：49
• 期：26
• 页码：7607 - 7610
• 全文大小：46K
• 年卷期：v.49,no.26(December 28, 2006)
• ISSN：1520-4804

文摘

In this work we describe the synthesis and biologicalevaluation of the tacrine-1,4-dihydropyridine (DHP) hybrids (3-11).These multipotent molecules are the result of the juxtaposition of anacetylcholinesterase inhibitor (AChEI) such as tacrine (1) and a 1,4-DHP such as nimodipine (2). Compounds 3-11 are very selective andpotent AChEIs and show an excellent neuprotective profile and amoderate Ca²⁺ channel blockade effect. Consequently, these moleculesare new potential drugs for the treatment of Alzheimer's disease.