Citation

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New 9-aminoacridine derivatives as inhibitors of botulinum neurotoxins and P. falciparum malaria

TOT, M;OPSENICA, DM;MITRIC, M;BURNETT, JC;GOMBA, L;BAVARI, S;OLAJA, BA;

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]