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Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships

Ahenkorah, S. and Coertzen, D. and Tong, J. X. and Fridianto, K. and Wittlin, S. and Birkholtz, L. M. and Tan, K. S. W. and Lam, Y. and Go, M. L. and Haynes, R. K.. (2020) Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships. ACS medicinal chemistry letters, 11. pp. 49-55.

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Official URL: https://edoc.unibas.ch/75569/

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Abstract

Here we report the nanomolar potencies of N (1),N (3)-dialkyldioxonaphthoimidazoliums against asexual forms of sensitive and resistant Plasmodium falciparum. Activity was dependent on the presence of the fused quinone-imidazolium entity and lipophilicity imparted by the N(1)/N(3) alkyl residues on the scaffold. Gametocytocidal activity was also detected, with most members active at IC50 < 1 muM. A representative analog with good solubility, limited PAMPA permeability, and microsomal stability demonstrated oral efficacy on a humanized mouse model of P. falciparum.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Article Subtype:Further Journal Contribution
Publisher:American Chemical Society
ISSN:1948-5875
Note:Publication type according to Uni Basel Research Database: Journal item
Identification Number:
Last Modified:05 Mar 2020 09:38
Deposited On:05 Mar 2020 09:38

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