Document Report Card

ID: ALA1155893

Journal: J Med Chem

Title: Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A.

Authors: Solaja BA, Opsenica D, Smith KS, Milhous WK, Terzić N, Opsenica I, Burnett JC, Nuss J, Gussio R, Bavari S.

Abstract: We report on the initial result of the coupling of 4-amino-7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low micromolar levels (7-31 microM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.

CiteXplore: 18637666

DOI: 10.1021/jm800737y