title: Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids.
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.
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil.
authors.forename: Luiz C S
authors.initials: LC
authors.lastname: Pinheiro
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil. Electronic address: boechat@far.fiocruz.br.
authors.forename: Núbia
authors.initials: N
authors.lastname: Boechat
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil.
authors.forename: Maria de Lourdes G
authors.initials: Mde L
authors.lastname: Ferreira
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil; Programa de Pós Graduação em Farmacologia e Química Medicinal, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Carlos C S
authors.initials: CC
authors.lastname: Júnior
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil.
authors.forename: Antônio M L
authors.initials: AM
authors.lastname: Jesus
authors.affiliation: Departamento de Síntese de Fármacos, Instituto de Tecnologia em Fármacos, Farmanguinhos-FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, RJ 21041-250, Brazil.
authors.forename: Milene M M
authors.initials: MM
authors.lastname: Leite
authors.affiliation: Centro de Pesquisas René Rachou, CPqRR-FIOCRUZ, Belo Horizonte, MG 30190-002, Brazil.
authors.forename: Nicolli B
authors.initials: NB
authors.lastname: Souza
authors.affiliation: 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: akrettli@cpqrr.fiocruz.br.
authors.forename: Antoniana U
authors.initials: AU
authors.lastname: Krettli
mesh_terms: D000818:Animals; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000627:therapeutic use*; D013449:Sulfonamides / Q000627:therapeutic use
chemical_list: D011804:Quinolines; D013449:Sulfonamides; C037219:quinoline
keywords: Hybrids; Malaria; Plasmodium falciparum; Quinoline; Sulfonamide