Приказ основних података о документу
New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria
Novi derivati 9-aminoakridina kao inhibitori botulinum neurotoksina i P. falciparum parazita malarije
dc.creator | Tot, Miklos | |
dc.creator | Opsenica, Dejan | |
dc.creator | Mitrić, Milena | |
dc.creator | Burnett, James C. | |
dc.creator | Gomba, Laura | |
dc.creator | Bavari, Sina | |
dc.creator | Šolaja, Bogdan | |
dc.date.accessioned | 2019-01-30T17:35:14Z | |
dc.date.available | 2019-01-30T17:35:14Z | |
dc.date.issued | 2013 | |
dc.identifier.issn | 0352-5139 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/1229 | |
dc.description.abstract | Steroidal 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.abstract | Sintetisani 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.publisher | Serbian Chemical Soc, Belgrade | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.source | Journal of the Serbian Chemical Society | |
dc.subject | antiviral | en |
dc.subject | BoNT/A | en |
dc.subject | BoNT/B | en |
dc.subject | antimalarial | en |
dc.subject | aminoacridine | en |
dc.title | New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria | en |
dc.title | Novi derivati 9-aminoakridina kao inhibitori botulinum neurotoksina i P. falciparum parazita malarije | sr |
dc.type | article | |
dc.rights.license | BY-NC-ND | |
dcterms.abstract | Опсеница, 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.volume | 78 | |
dc.citation.issue | 12 | |
dc.citation.spage | 1847 | |
dc.citation.epage | 1864 | |
dc.citation.other | 78(12): 1847-1864 | |
dc.citation.rank | M23 | |
dc.identifier.doi | 10.2298/JSC130924112T | |
dc.identifier.fulltext | https://cer.ihtm.bg.ac.rs//bitstream/id/7742/1227.pdf | |
dc.identifier.scopus | 2-s2.0-84890853204 | |
dc.identifier.wos | 000329261200003 | |
dc.type.version | publishedVersion |