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• W2895049743 abstract "This paper describes the synthesis and anticholinesterase potency of Cinchona-based alkaloids; ten quaternary derivatives of cinchonines and their corresponding pseudo-enantiomeric cinchonidines. The quaternization of quinuclidine moiety of each compound was carried out with groups diverse in their size: methyl, benzyl and differently meta- and para-substituted benzyl groups. All of the prepared compounds reversibly inhibited human butyrylcholinesterase and acetylcholinesterase with Ki constants within nanomolar to micromolar range. Five cinchonidine derivatives displayed 95-510 times higher inhibition selectivity to butyrylcholinesterase over acetylcholinesterase and four were potent butyrylcholinesterase inhibitors with Ki constants up to 100 nM, of which N-para-bromobenzyl cinchonidinium bromide can be considered a lead for further modifications and optimizations for possible use in the treatment of neurodegenerative diseases." @default.
• W2895049743 created "2018-10-12" @default.
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• W2895049743 date "2018-10-05" @default.
• W2895049743 modified "2023-10-18" @default.
• W2895049743 title "Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold" @default.
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• W2895049743 doi "https://doi.org/10.1371/journal.pone.0205193" @default.
• W2895049743 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6173406" @default.
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