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Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold [Elektronski vir]Bosak, Anita ...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.Source: PloS one [Elektronski vir]. - ISSN 1932-6203 (Vol. 13, iss. 10, Oct. 2018, str. 1-18)Type of material - e-articlePublish date - 2018Language - englishCOBISS.SI-ID - 34248153
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Bosak, Anita | 52614 |
Ramić, Alma | ![]() |
Šmidlehner, Tamara | 53047 |
Hrenar, Tomica | ![]() |
Primožič, Ines | ![]() |
Kovarik, Zrinka | ![]() |
Source: Personal bibliographies
and: SICRIS
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