TY  - JOUR
AU  - Tot, Mikloš
AU  - Opsenica, Dejan M.
AU  - Mitric, Milena
AU  - Burnett, James C.
AU  - Gomba, Laura
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2013
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/1461
AB  - 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 gt 326), indicating that an adamantyl group is a better carrier than a steroidal motif for this indication.
AB  - 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  gt  326), pokazujući da je adamantil-grupa bolji nosač farmakofore u poređenju sa steroidnim, prema ovoj indikaciji. .
PB  - Serbian Chemical Soc, Belgrade
T2  - Journal of the Serbian Chemical Society
T1  - New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria
T1  - Novi derivati 9-aminoakridina kao inhibitori botulinum neurotoksina i P. falciparum parazita malarije
VL  - 78
IS  - 12
SP  - 1847
EP  - 1864
DO  - 10.2298/JSC130924112T
ER  - 

@article{
author = "Tot, Mikloš and Opsenica, Dejan M. and Mitric, Milena and Burnett, James C. and Gomba, Laura and Bavari, Sina and Šolaja, Bogdan A.",
year = "2013",
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 gt 326), indicating that an adamantyl group is a better carrier than a steroidal motif for this indication., 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  gt  326), pokazujući da je adamantil-grupa bolji nosač farmakofore u poređenju sa steroidnim, prema ovoj indikaciji. .",
publisher = "Serbian Chemical Soc, Belgrade",
journal = "Journal of the Serbian Chemical Society",
title = "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",
volume = "78",
number = "12",
pages = "1847-1864",
doi = "10.2298/JSC130924112T"
}

Tot, M., Opsenica, D. M., Mitric, M., Burnett, J. C., Gomba, L., Bavari, S.,& Šolaja, B. A.. (2013). New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria. in Journal of the Serbian Chemical Society
Serbian Chemical Soc, Belgrade., 78(12), 1847-1864.
https://doi.org/10.2298/JSC130924112T

Tot M, Opsenica DM, Mitric M, Burnett JC, Gomba L, Bavari S, Šolaja BA. New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria. in Journal of the Serbian Chemical Society. 2013;78(12):1847-1864.
doi:10.2298/JSC130924112T .

Tot, Mikloš, Opsenica, Dejan M., Mitric, Milena, Burnett, James C., Gomba, Laura, Bavari, Sina, Šolaja, Bogdan A., "New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria" in Journal of the Serbian Chemical Society, 78, no. 12 (2013):1847-1864,
https://doi.org/10.2298/JSC130924112T . .