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Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids. | LitMetric

Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids.

Bioorg Med Chem

Centro de Pesquisas René Rachou, CPqRR-FIOCRUZ, Belo Horizonte, MG 30190-002, Brazil; Programa de Pós Graduação em Medicina Molecular, Faculdade de Medicina, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil. Electronic address:

Published: September 2015

AI Article Synopsis

Article Abstract

Fifteen quinoline-sulfonamide hybrids, with a 7-chloroquinoline moiety connected by a linker group to arylsulfonamide moieties with different substituents in the 4-position were synthesized and assayed against Plasmodium falciparum. The compounds displayed high schizonticidal blood activity in vitro, with IC50 values ranging from 0.05 to 1.63 μM, in the anti-HPR2 assay against clone W2-chloroquine-resistant; ten of them showed an IC50 (ranging from 0.05 to 0.40 μM) lower than that of chloroquine and sulfadoxine. Among them, two compounds inhibited Plasmodium berghei parasitemia by 47% and 49% on day 5 after mice inoculation. The most active, in vivo, hybrid 13 is considered to be a new prototype for the development of an antimalarial drug against chloroquine-resistant parasites.

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Source
http://dx.doi.org/10.1016/j.bmc.2015.06.056DOI Listing

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