Nalazite se na CroRIS probnoj okolini. Ovdje evidentirani podaci neće biti pohranjeni u Informacijskom sustavu znanosti RH. Ako je ovo greška, CroRIS produkcijskoj okolini moguće je pristupi putem poveznice www.croris.hr
izvor podataka: crosbi

Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold (CROSBI ID 254627)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

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, - (2018), e0205193, 11. doi: 10.1371/journal.pone.0205193

Podaci o odgovornosti

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

engleski

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

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

cinchonine, cinchonidine, selectivity, stereoselectivity, inhibition constants

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

Podaci o izdanju

-

2018.

e0205193

11

objavljeno

1932-6203

10.1371/journal.pone.0205193

Povezanost rada

Kemija

Poveznice
Indeksiranost