Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 3, Pages 1400-1419Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm501722s
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Funding
- Agency for Science Technology and Research (A*STAR) [1021490113]
- Hungarian Office of Science and Technology [TET_10-1-2011-0050]
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To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamine oxidases. From this, a number of highly potent and selective monoamine oxidase B inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively. It was observed that some of the compounds tested yielded a marked increase in survival in PC-12 cells treated with the neurotoxins. This indicates that these propargylamines are able to confer protection against the effects of the toxins and may also be considered as novel disease-modifying anti-Parkinsonian agents, which are much needed for the therapy of Parkinson's disease.
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