Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids

被引：30

作者：

Pinheiro, Luiz C. S. ^{[1
]}

Boechat, Nubia ^{[1
]}

Ferreira, Maria de Lourdes G. ^{[1
]}

Junior, Carlos C. S. ^{[1
,2
]}

Jesus, Antonio M. L. ^{[1
]}

Leite, Milene M. M. ^{[1
]}

Souza, Nicolli B. ^{[3
]}

Krettli, Antoniana U. ^{[3
,4
]}

机构：

[1] Farmanguinhos FIOCRUZ, Inst Tecnol Farm, Dept Sintese Farm, BR-21041250 Rio De Janeiro, RJ, Brazil

[2] Univ Fed Rio de Janeiro, Inst Ciencias Biomed, Programa Pos Grad Farmacol & Quim Med, Rio De Janeiro, RJ, Brazil

[3] CPqRR FIOCRUZ, Ctr Pesquisas Rene Rachou, BR-30190002 Belo Horizonte, MG, Brazil

[4] Univ Fed Minas Gerais, Fac Med, Programa Pos Grad Med Mol, Belo Horizonte, MG, Brazil

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 17期

关键词：

Malaria; Quinoline; Sulfonamide; Hybrids; Plasmodium falciparum; ANTIMALARIAL-DRUGS; MALARIA; DESIGN; MODE; ANALOGS;

D O I：

10.1016/j.bmc.2015.06.056

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M, in the anti-HPR2 assay against clone W2-chloroquine-resistant; ten of them showed an IC50 (ranging from 0.05 to 0.40 mu M) 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. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：5979 / 5984

页数：6

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