Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease

Paul B. Huleatt, Mui Ling Khoo, Yi Yuan Chua, Tiong Wei Tan, Rou Shen Liew, Balázs Balogh, Ruth Deme, Flóra Gölöncsér, Kalman Magyar, David P. Sheela, Han Kiat Ho, Beáta Sperlágh, Péter Mátyus, Christina L.L. Chai

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22 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1400-1419
Number of pages20
JournalJournal of Medicinal Chemistry
Volume58
Issue number3
DOIs
Publication statusPublished - Feb 12 2015

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Huleatt, P. B., Khoo, M. L., Chua, Y. Y., Tan, T. W., Liew, R. S., Balogh, B., Deme, R., Gölöncsér, F., Magyar, K., Sheela, D. P., Ho, H. K., Sperlágh, B., Mátyus, P., & Chai, C. L. L. (2015). Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease. Journal of Medicinal Chemistry, 58(3), 1400-1419. https://doi.org/10.1021/jm501722s