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4-Aminoqionolines as reversible inhibitors of human cholinesterase activity

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2018
954584.MMSL_mms-201888-0083.pdf (65.10Kb)
Autori
Bosak, Anita
Opsenica, Dejan
Šinko, Goran
Zlatar, Matija
Kovarik, Zrinka
Konferencijski prilog (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentu
Apstrakt
We synthesised eight derivatives of 4-aminoquinolines differing in the substituents attached to the C(4)-amino group and C(7) carbon of 4-aminoquinoline, and tested their potency to inhibit human AChE and BChE. All of the compounds reversibly inhibited both enzymes with dissociation inhibition (Ki) constants from 0.50 to 50 µM exhibiting selectivity. In other words, for all compounds, AChE exhibited higher affinity than BChE. The most potent inhibitors of AChE were compounds with an octyl chain or adamantane, regardless of the group in position C(7). The shortening of the chain length caused the AChE inhibition decrease by 5-20 times. Docking studies made it clear that the high AChE affinity resulted from simultaneous interactions of the quinoline group with aromatic residues of both the catalytic active site and the peripheral site. In conclusion, the inhibition potency and selectivity classify several novel compounds as leads for further modification and optimization towards the deve...lopment of new inhibitors of AChE and potential drugs for treatment of neurodegenerative diseases.

Ključne reči:
acetylcholinesterase / butyrylcholinesterase / treatment / 4-aminoquinoline / Alzheimer’s disease / Docking
Izvor:
Military Medical Science Letters, 2018, 87, Suppl. 1, 83-83
Izdavač:
  • Faculty of Military Health Sciences, Czech Republic
Projekti:
  • Sinteza aminohinolina i njihovih derivata kao antimalarika i inhibitora botulinum neurotoksina A (RS-172008)
  • Racionalni dizajn i sinteza biološki aktivnih i koordinacionih jedinjenja i funkcionalnih materijala, relevantnih u (bio)nanotehnologiji (RS-172035)
Napomena:
  • 13th International Meeting on Cholinesterases and and the 7th International Conference on Paraoxonases, 9th to 14th of September 2018 Hradec Králové, Czech Republic

ISSN: 0372-7025

[ Google Scholar ]
URI
https://mmsl.cz/artkey/mms-201888-0083.php
http://cer.ihtm.bg.ac.rs/handle/123456789/3216
Kolekcije
  • Radovi istraživača / Researchers' publications
Institucija
IHTM

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