Idioma:

Anti-Plasmodium falciparum activity of quinoline–sulfonamide hybrids

Pinheiro, Luiz C.S. ; Boechat, Núbia ; Ferreira, Maria de Lourdes G. ; Júnior, Carlos C.S. ; Jesus, Antônio M.L. ; Leite, Milene M.M. ; Souza, Nicolli B. ; Krettli, Antoniana U.

Bioorganic & medicinal chemistry, 2015-09, Vol.23 (17), p.5979-5984 [Periódico revisado por pares]

England: Elsevier Ltd

Texto completo disponível

Citações Citado por

Enviar para

Título:
Anti-Plasmodium falciparum activity of quinoline–sulfonamide hybrids
Autor: Pinheiro, Luiz C.S. ; Boechat, Núbia ; Ferreira, Maria de Lourdes G. ; Júnior, Carlos C.S. ; Jesus, Antônio M.L. ; Leite, Milene M.M. ; Souza, Nicolli B. ; Krettli, Antoniana U.
Assuntos: Animals ; Humans ; Hybrids ; Malaria ; Malaria - drug therapy ; Mice ; Molecular Structure ; Plasmodium falciparum ; Plasmodium falciparum - drug effects ; Quinoline ; Quinolines - therapeutic use ; Sulfonamide ; Sulfonamides - therapeutic use
É parte de: Bioorganic & medicinal chemistry, 2015-09, Vol.23 (17), p.5979-5984
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: [Display omitted] 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 1.63μM, in the anti-HPR2 assay against clone W2-chloroquine-resistant; ten of them showed an IC50 (ranging from 0.05 to 0.40μM) 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.
Editor: England: Elsevier Ltd
Idioma: Inglês

Links

View this record in MEDLINE/PubMed

Voltar para lista de resultados

Realização: Logos de Redes Sociais:

Anti-Plasmodium falciparum activity of quinoline–sulfonamide hybrids

Pinheiro, Luiz C.S. ; Boechat, Núbia ; Ferreira, Maria de Lourdes G. ; Júnior, Carlos C.S. ; Jesus, Antônio M.L. ; Leite, Milene M.M. ; Souza, Nicolli B. ; Krettli, Antoniana U.

England: Elsevier Ltd

Buscando em bases de dados remotas. Favor aguardar.