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羟乙基哌嗪衍生物的合成及其抗疟活性

Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives.

作者信息

Cunico Wilson, Gomes Claudia R B, Moreth Marcele, Manhanini Diogo P, Figueiredo Isabela H, Penido Carmen, Henriques Maria G M O, Varotti Fernando P, Krettli Antoniana U

机构信息

Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos, Farmanguinhos R. Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.

出版信息

Eur J Med Chem. 2009 Mar;44(3):1363-8. doi: 10.1016/j.ejmech.2008.04.009. Epub 2008 Apr 29.

DOI:10.1016/j.ejmech.2008.04.009
PMID:18514971
Abstract

The antimalarial activity of hydroxyethylpiperazine derivatives, synthesized from the reaction of (2S,3S)Boc-phenylalanine 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 microg/ml).

摘要

由(2S,3S)-Boc-苯丙氨酸环氧化物与苄基哌嗪反应以良好产率(76 - 96%)合成的羟乙基哌嗪衍生物的抗疟活性已在体外针对恶性疟原虫W2克隆(氯喹耐药)进行了评估。结果表明,一些化合物对该寄生虫具有中等活性,且所有活性化合物在高浓度(100微克/毫升)时均未显示出细胞毒性。

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