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dc.creatorBosak, Anita
dc.creatorOpsenica, Dejan
dc.creatorŠinko, Goran
dc.creatorZlatar, Matija
dc.creatorKovarik, Zrinka
dc.date.accessioned2019-11-27T22:42:44Z
dc.date.available2019-11-27T22:42:44Z
dc.date.issued2018
dc.identifier.issn0372-7025
dc.identifier.urihttps://mmsl.cz/artkey/mms-201888-0083.php
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/3216
dc.description.abstractWe 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 development of new inhibitors of AChE and potential drugs for treatment of neurodegenerative diseases.
dc.publisherFaculty of Military Health Sciences, Czech Republic
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172035/RS//
dc.rightsopenAccess
dc.sourceMilitary Medical Science Letters
dc.subjectacetylcholinesterase
dc.subjectbutyrylcholinesterase
dc.subjecttreatment
dc.subject4-aminoquinoline
dc.subjectAlzheimer’s disease
dc.subjectDocking
dc.title4-Aminoqionolines as reversible inhibitors of human cholinesterase activity
dc.typeconferenceObject
dc.rights.licenseARR
dcterms.abstractБосак, Aнита; Шинко, Горан; Коварик, Зринка; Опсеница, Дејан; Златар, Матија;
dc.citation.volume87
dc.citation.issueSuppl. 1
dc.citation.spage83
dc.citation.epage83
dc.description.other13th International Meeting on Cholinesterases and and the 7th International Conference on Paraoxonases, 9th to 14th of September 2018 Hradec Králové, Czech Republic
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs/bitstream/id/15493/954584.MMSL_mms-201888-0083.pdf
dc.type.versionpublishedVersion


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