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American Chemical Society, Journal of Medicinal Chemistry, 26(49), p. 7607-7610, 2006

DOI: 10.1021/jm061047j

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

Journal article published in 2006 by José Marco-Contelles, Rafael León, Cristóbal de Los Ríos ORCID, Antonio Guglietta, José Terencio, Manuela G. López ORCID, Antonio G. García,‡,# And, Antonio G. García, Mercedes Villarroya
This paper is available in a repository.
This paper is available in a repository.

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Abstract

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