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Issue 1, 2017
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Synthesis and biological evaluation of memantine nitrates as a potential treatment for neurodegenerative diseases

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Abstract

A series of memantine nitrate derivatives, as dual functional compounds with neuroprotective and vasodilatory activity for neurodegenerative diseases, was designed and synthesized. These compounds combined the memantine skeleton and a nitrate moiety, and thus inhibited the N-methyl-D-aspartic acid receptor and released NO in the central nervous system. The biological evaluation results revealed that the new memantine nitrates were effective in protecting neurons against glutamate-induced injury in vitro. Moreover, memantine nitrates dilated aortic rings against phenylephrine-induced contraction. The structure–activity relationships of neuroprotection and vasodilation were both analyzed. In further studies, compound MN-05 significantly protected cortical neurons by inhibiting Ca2+ influx, reducing free radical production and maintaining the mitochondrial membrane potential. Further research on MN-05 is warranted.

Graphical abstract: Synthesis and biological evaluation of memantine nitrates as a potential treatment for neurodegenerative diseases

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Publication details

The article was received on 05 Sep 2016, accepted on 18 Oct 2016 and first published on 20 Oct 2016


Article type: Research Article
DOI: 10.1039/C6MD00509H
Citation: Med. Chem. Commun., 2017,8, 135-147
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    Synthesis and biological evaluation of memantine nitrates as a potential treatment for neurodegenerative diseases

    Z. Liu, S. Yang, X. Jin, G. Zhang, B. Guo, H. Chen, P. Yu, Y. Sun, Z. Zhang and Y. Wang, Med. Chem. Commun., 2017, 8, 135
    DOI: 10.1039/C6MD00509H

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