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Pregled bibliografske jedinice broj: 954675

Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold


Bosak, Anita; Ramić, Alma; Šmidlehner, Tamara; Hrenar, Tomica; Primožič, Ines; Kovarik, Zrinka
Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold // PLoS One, 1 (2018), 1; 1-18 doi:10.1371/journal.pone.0205193 (međunarodna recenzija, članak, znanstveni)


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Naslov
Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold

Autori
Bosak, Anita ; Ramić, Alma ; Šmidlehner, Tamara ; Hrenar, Tomica ; Primožič, Ines ; Kovarik, Zrinka

Izvornik
PLoS One (1932-6203) 1 (2018), 1; 1-18

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants

Sažetak
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 K(I) 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

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekti:
HRZZ-IP-2016-06-3775 - Aktivnošću i in silico usmjeren dizajn malih bioaktivnih molekula (ADESIRE) (Hrenar, Tomica, HRZZ - 2016-06) ( POIROT)
IP-2013-11-4307 - Dizajn, sinteza i evaluacija novih protuotrova kod trovanja živčanim bojnim otrovima i pesticidima (CHOLINESTERASE) (Kovarik, Zrinka, HRZZ - 2013-11) ( POIROT)

Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb,
Prirodoslovno-matematički fakultet, Zagreb

Profili:

Avatar Url Tamara Šmidlehner (autor)

Avatar Url Ines Primožič (autor)

Avatar Url Alma Ramic (autor)

Avatar Url Zrinka Kovarik (autor)

Avatar Url Tomica Hrenar (autor)

Avatar Url Anita Bosak (autor)

Citiraj ovu publikaciju

Bosak, Anita; Ramić, Alma; Šmidlehner, Tamara; Hrenar, Tomica; Primožič, Ines; Kovarik, Zrinka
Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold // PLoS One, 1 (2018), 1; 1-18 doi:10.1371/journal.pone.0205193 (međunarodna recenzija, članak, znanstveni)
Bosak, A., Ramić, A., Šmidlehner, T., Hrenar, T., Primožič, I. & Kovarik, Z. (2018) Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold. PLoS One, 1 (1), 1-18 doi:10.1371/journal.pone.0205193.
@article{article, year = {2018}, pages = {1-18}, DOI = {10.1371/journal.pone.0205193}, keywords = {cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants}, journal = {PLoS One}, doi = {10.1371/journal.pone.0205193}, volume = {1}, number = {1}, issn = {1932-6203}, title = {Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold}, keyword = {cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants} }
@article{article, year = {2018}, pages = {1-18}, DOI = {10.1371/journal.pone.0205193}, keywords = {cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants}, journal = {PLoS One}, doi = {10.1371/journal.pone.0205193}, volume = {1}, number = {1}, issn = {1932-6203}, title = {Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold}, keyword = {cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants} }

Časopis indeksira:


  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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