Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives

被引：47

作者：

Cunico, Wilson ^{[1
]}

Gomes, Claudia R. B. ^{[1
]}

Moreth, Marcele ^{[1
]}

Manhanini, Diogo P. ^{[1
,2
]}

Figueiredo, Isabela H. ^{[2
]}

Penido, Carmen ^{[2
]}

Henriques, Maria G. M. O. ^{[2
]}

Varotti, Fernando P. ^{[3
,4
]}

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

机构：

[1] Inst Tecnol Farmacos, Fundacao Oswaldo Cruz, BR-21041250 Rio De Janeiro, Brazil

[2] Inst Tecnol Farmacos, Dept Farmacol Aplicada, BR-21041250 Rio De Janeiro, Brazil

[3] Fiocruz MS, Ctr Pesquisas Rene Rachou, Belo Horizonte, MG, Brazil

[4] Univ Fed Minas Gerais, Dept Parasitol, Belo Horizonte, MG, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 03期

关键词：

Hydroxyethylpiperazine; Malaria; Piperazine; HIV-PROTEASE INHIBITORS; PLASMODIUM-FALCIPARUM; PLASMEPSIN-II; ASPARTIC PROTEASES; ACTIVITY INVITRO; MALARIA; CULTURE; DESIGN; POTENT; AGENTS;

D O I：

10.1016/j.ejmech.2008.04.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The antimalarial activity of hydroxyethylpiperazine derivatives, synthesized from the reaction of (2S,3S)Boc-phenylaianine epoxide with benzylpiperazines in good yields (76-96%), has been evaluated in vitro against the Plasmodium falciparum W2 clone (chloroquine resistant). The results show that some compounds have moderate activity against this parasite and none of the active compounds showed cytotoxicity at high concentration (100 mu g/ml). (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：1363 / 1368

页数：6

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