Property | Value |
Name | Probe to Bifunctional Memantine Derivatives for Treatment of Alzheimer's Disease |
Description | Original article
ABSTRACT: Alzheimer’ disease (AD) is a neurodegenerative disease commonly occurring in older people. Two types of drugs, the acetylcholinesterase (AChE) inhibitor and the N-methyl-D-aspartate receptor (NMDAR) antagonist, were approved to treat AD by FDA. Of them, memantine was the only one of NMDAR antagonist. Previous studies had revealed that the carbamate grouphad a better AChE inhibitor activity. Herein, a series of new memantine derivatives with a carbamate group were designed and synthesized. They were expected to haveboth NMDAR antagonism and AChE inhibition. However, the neuroprotective effect of these new compounds against the glutamate-induced neurotoxicity was not as effective as memantine. The AChE inhibition of them wasalso lower than tacrine. The combine of memantine moiety and carbamate group attenuated the activities of the two functional groups. It may be caused by the changes of the spatial structures after combination. The introduction of large spatial structures makes the functional groups difficult to orientate to the active site. |
Filename | Zheng Liu(276-290).pdf |
Filesize | 538.17 kB |
Filetype | pdf (Mime Type: application/pdf) |
Creator | admin |
Created On: | 04/16/2015 00:00 |
Viewers | Everybody |
Maintained by | Editor |
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Last updated on | 04/27/2015 13:21 |
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