title: Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
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.
authors: Institute of Chemical and Engineering Sciences , A* STAR (Agency of Science, Technology and Research), 8 Biomedical Grove, Neuros #07-01, Singapore 138665, Singapore.
authors: Paul B
authors: PB
authors: Huleatt
authors: Mui Ling
authors: ML
authors: Khoo
authors: Yi Yuan
authors: YY
authors: Chua
authors: Tiong Wei
authors: TW
authors: Tan
authors: Rou Shen
authors: RS
authors: Liew
authors: Balázs
authors: B
authors: Balogh
authors: Ruth
authors: R
authors: Deme
authors: Flóra
authors: F
authors: Gölöncsér
authors: Kalman
authors: K
authors: Magyar
authors: David P
authors: DP
authors: Sheela
authors: Han Kiat
authors: HK
authors: Ho
authors: Beáta
authors: B
authors: Sperlágh
authors: Péter
authors: P
authors: Mátyus
authors: Christina L L
authors: CL
authors: Chai
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016716:PC12 Cells; D010293:Pargyline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010300:Parkinson Disease / Q000188:drug therapy* / Q000201:enzymology / Q000378:metabolism; D011437:Propylamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D008996:Monoamine Oxidase Inhibitors; D018696:Neuroprotective Agents; D011437:Propylamines; C009054:propargylamine; D010293:Pargyline; D008995:Monoamine Oxidase