85277-62-9Relevant academic research and scientific papers
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease
Huleatt, Paul B.,Khoo, Mui Ling,Chua, Yi Yuan,Tan, Tiong Wei,Liew, Rou Shen,Balogh, Balázs,Deme, Ruth,G?l?ncsér, Flóra,Magyar, Kalman,Sheela, David P.,Ho, Han Kiat,Sperlágh, Beáta,Mátyus, Péter,Chai, Christina L. L.
supporting information, p. 1400 - 1419 (2015/03/04)
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.
NEW ARYLALKENYLPROPARGYLAMINE DERIVATIVES EXHIBITING NEUROPROTECTIVE ACTION FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Page/Page column 96, (2015/06/25)
The invention relates to novel arylalkenylpropargylamine derivatives of general formula (I) or enantiomers or diastereomers thereof or salts, optionally pharmaceutically acceptable salts, or solvates of any of these. The compounds can be used in treating or preventing a disease or condition in a mammal related to monoamine oxidase dysfunction, especially in neurodegenerative diseases, e.g. Parkinson's disease, Alzheimer's disease or Huntington's disease.
Highly enantioselective synthesis of α,α-dialkylmalonates by phase-transfer catalytic desymmetrization
Hong, Suckchang,Lee, Jihye,Kim, Minsik,Park, Yohan,Park, Cheonhyoung,Kim, Mi-Hyun,Jew, Sang-Sup,Park, Hyeung-Geun
supporting information; experimental part, p. 4924 - 4929 (2011/06/10)
A novel enantioselective synthetic method for the construction of a quaternary carbon center from malonates via phase-transfer catalytic (PTC) alkylation has been developed. The asymmetric α-alkylation of diphenylmethyl tert-butyl α-alkylmalonates with alkylating agents under phase-transfer catalysis conditions (aq 50% KOH, toluene, 0°C) in the presence of (S,S)-3,4,5-trifluorophenyl-NAS bromide (8) as PTC catalyst afforded the corresponding α,α-dialkylmalonates in high chemical (up to 99%) and optical yields (up to 97% ee) which could be readily converted to versatile chiral intermediates. Notably, the direct double α-alkylations of diphenylmethyl tert-butyl malonate also provided the corresponding α,α-dialkylmalonates without loss of enantioselectivity. The synthetic potential of this method has been demonstrated by the preparation of α,α-dialkylamino acid and oxindole systems.
Palladium-catalyzed asymmetric decarboxylative lactamization of γ-methylidene-δ-valerolactones with isocyanates: Conversion of racemic lactones to enantioenriched lactams
Shintani, Ryo,Park, Soyoung,Shirozu, Fumitaka,Murakami, Masataka,Hayashi, Tamio
supporting information; experimental part, p. 16174 - 16175 (2009/05/09)
A palladium-catalyzed asymmetric decarboxylative reaction of racemic γ-methylidene-δ-valerolactones with aryl isocyanates has been developed to give enantioenriched 3,3-disubstituted 2-piperidones. High enantioselectivity has been achieved by tuning the e
Inactivation of bovine plasma amine oxidase by haloallylamines
Kim, Jisook,Zhang, Yuming,Ran, Chongzhao,Sayre, Lawrence M.
, p. 1444 - 1453 (2007/10/03)
Various 2- and 3-haloallylamines were synthesized and evaluated as inhibitors of the quinone-dependent bovine plasma amine oxidase (BPAO). 3-Haloallylamines, which were previously found to be good inhibitors of the flavin-dependent mitochondrial monoamine
Enzyme-activated irreversible inhibitors of monoamine oxidase: Phenylallylamine structure-activity relationships
McDonald,Lacoste,Bey,Palfreyman,Zreika
, p. 186 - 193 (2007/10/02)
Seventeen 2-aryl-3-haloallylamine derivatives were prepared and evaluated as inhibitors of monoamine oxidase (MAO, EC 1.4.3.4). The synthesis of these compounds was achieved from either α-methylstyrene or ring-substituted phenylacetic acid derivatives. Wi
