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Novi derivati 9-aminoakridina kao inhibitori botulinum neurotoksina i P. falciparum parazita malarije

dc.creatorTot, Miklos
dc.creatorOpsenica, Dejan
dc.creatorMitrić, Milena
dc.creatorBurnett, James C.
dc.creatorGomba, Laura
dc.creatorBavari, Sina
dc.creatorŠolaja, Bogdan
dc.date.accessioned2019-01-30T17:35:14Z
dc.date.available2019-01-30T17:35:14Z
dc.date.issued2013
dc.identifier.issn0352-5139
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/1229
dc.description.abstractSteroidal and adamantane aminoacridine derivatives were prepared and tested as both botulinum neurotoxin (BoNT) inhibitors and antimalarials. Steroid-bound acridines provided good potency against both the BoNT/A and BoNT/B light chains (LCs). The observed inhibition of the BoNT/B LC by ca. 50% is the highest attained inhibitory activity against this serotype by acridine-based compounds to date. With respect to the antimalarial activity, the adamantane acridines were the most potent derivatives (IC50 = 6-9 nM, SI > 326), indicating that an adamantyl group is a better carrier than a steroidal motif for this indication. .en
dc.description.abstractSintetisani su derivati steroidnih i adamantil-akridina i ispitana je njihova inhibitorna aktivnost prema botulinum neurotoksinima (BoNT) i parazitu malarije. Steroidni akridini pokazuju dobru inhibiciju prema kratkom nizu (LCs) BoNT/A i BoNT/B. Ostvarena inhibicija BoNT/B LC od oko 50% je najviša postignuta vrednost akridinskih derivata prema ovom serotipu. Adamantil-akridinski derivati su pokazali najveću antimalarijsku aktivnost (IC50 u opsegu 6-9 nM, SI > 326), pokazujući da je adamantil-grupa bolji nosač farmakofore u poređenju sa steroidnim, prema ovoj indikaciji. .sr
dc.publisherSerbian Chemical Soc, Belgrade
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.rightsopenAccess
dc.sourceJournal of the Serbian Chemical Society
dc.subjectantiviralen
dc.subjectBoNT/Aen
dc.subjectBoNT/Ben
dc.subjectantimalarialen
dc.subjectaminoacridineen
dc.titleNew 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malariaen
dc.titleNovi derivati 9-aminoakridina kao inhibitori botulinum neurotoksina i P. falciparum parazita malarijesr
dc.typearticle
dc.rights.licenseBY-NC-ND
dcterms.abstractОпсеница, Дејан; Митрић, Милена; Бурнетт, Јамес Ц.; Бавари, Сина; Тот, Миклос; Гомба, Лаура; Солаја, Богдан A.; Нови деривати 9-аминоакридина као инхибитори ботулинум неуротоксина и П. фалципарум паразита маларије; Нови деривати 9-аминоакридина као инхибитори ботулинум неуротоксина и П. фалципарум паразита маларије;
dc.citation.volume78
dc.citation.issue12
dc.citation.spage1847
dc.citation.epage1864
dc.citation.other78(12): 1847-1864
dc.citation.rankM23
dc.identifier.doi10.2298/JSC130924112T
dc.identifier.rcubConv_3086
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs//bitstream/id/7742/1227.pdf
dc.identifier.scopus2-s2.0-84890853204
dc.identifier.wos000329261200003
dc.type.versionpublishedVersion


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