New 9-aminoacridine derivatives as inhibitors of Botulinum neurotoxins and P. falciparum malaria
| Autor: | Tot Mikloš, Opsenica Dejan M., Mitrić Milena, Burnett James C., Gomba Laura, Bavari Sina, Šolaja Bogdan A. |
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| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: | |
| Zdroj: | Journal of the Serbian Chemical Society, Vol 78, Iss 12, Pp 1847-1864 (2013) |
| Druh dokumentu: | article |
| ISSN: | 0352-5139 1820-7421 |
| DOI: | 10.2298/JSC130924112T |
| Popis: | 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 antimalarial activity, adamantane acridines were the most potent derivatives (IC50 = 6-9 nM, SI > 326), indicating that an adamantyl group is a better carries than a steroidal motif for this indication. [Projekat Ministarstva nauke Republike Srbije, br. 172008] |
| Databáze: | Directory of Open Access Journals |
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