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2,4-DIAMINO-6-ETHYLPYRIMIDINE DERIVATIVES WITH ANTIMALARIAL ACTIVITIES AGAINST PLASMODIUM FALCIPARUM

机译：具有抗恶性疟原虫活性的2,4-二氨基-6-乙啶嘧啶衍生物

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摘要

The present invention relates to 2,4-diamino-6-ethylpyrimidine derivatives that are inhibitors of wild type and quadruple mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum. They also show in vitro antimalarial activities against Plasmodium falciparum for both wild type and mutant that are comparable to or better than pyrimethamine. In addition, the compounds of the present invention show a good selectivity to Plasmodium falciparum and exhibit lower cytotoxicity than pyrimethamine.

机译：本发明涉及2，4-二氨基-6-乙基嘧啶衍生物，它们是野生型和恶性疟原虫的四重突变二氢叶酸还原酶（DHFR）的抑制剂。它们还显示出对野生型和突变型恶性疟原虫的体外抗疟活性，可与乙胺嘧啶相媲美或更好。此外，本发明的化合物对恶性疟原虫具有良好的选择性，并且比乙胺嘧啶具有较低的细胞毒性。 展开▼

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公开/公告号US2020239445A1

专利类型

公开/公告日2020-07-30

原文格式PDF

申请/专利权人 NATIONAL SCIENCE AND TECHNOLOGY DEVELOPMENT AGENCY;
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申请/专利号US201615762530

发明设计人 SUMALEE KAMCHONWONGPAISAN;NETNAPA CHAROENSETAKUL;KRISANA PEEWASAN;JARUNEE VANICHTANANKUL;ROONGLAWAN RATTANAJAK;SUPANNEE TAWEECHAI;TOSAPOL ANUKUNWITHAYA;APHISIT YOOMUANG;YONGYUTH YUTHAVONG;TIRAYUT VILAIVAN;
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申请日2016-09-16

分类号C07D403/04;C07D413/12;C07D417/12;A61P33/06;

国家 US

入库时间 2022-08-21 11:22:35

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机译： 2,4-二氨基-6-乙基嘧啶衍生物，对抗疟疾活性的衍生物对抗疟原虫（Plasmodium falciparum）

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机译：具有抗恶性疟原虫活性的2,4-二氨基-6-乙基嘧啶衍生物

5. 2,4-DIAMINO-6-ETHYLPYRIMIDINE DERIVATIVES WITH ANTIMALARIAL ACTIVITIES AGAINST PLASMODIUM FALCIPARUM [P] . 世界知识产权组织专利： WO2017052479A1 . 2017-03-30

机译：具有抗恶性疟原虫活性的2,4-二氨基-6-乙基嘧啶衍生物

1. In vitro Potentiation of Antimalarial Activities by Daphnetin Derivatives Against Plasmodium falciparum [J] . FANG HUANG, LIN-HUA TANG, LIN-QIAN YU, 生物医学与环境科学（英文版） . 2006,第005期

2. Structural features of substituted triazole-linked chalcone derivatives as antimalarial activities against D10 strains ofPlasmodium falciparum：A QSAR approach [J] . Mukesh C. Sharma 中南大学学报（英文版） . 2015,第010期

3. Effects of derivatives of human glycophorin A and their antibodies on the recognition and invasion of Plasmodium falciparum into erythrocytes [J] . 王向东, 骆训懿, 李建新, 中国人民解放军军医大学学报：英文版 . 1992,第001期

4. Antimalarial activity of the aqueous extract of Euphorbia cordifolia Elliot in Plasmodium berghei-infected mice [J] . Raceline Gounoue Kamkumo, Jaures Marius Tsakem Nangap, Lauve Rachel Tchokouaha Yamthe, 亚太热带医药杂志（英文版） . 2020,第004期

5. New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo [J] . Soares Roberta Reis, Fernandes da Silva Jose Marcio, Carlos Bianca Cecheto, Bioorganic and Medicinal Chemistry Letters . 2015,第11期

6. Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. [J] . de Andrade Neto VF, Goulart MO, da Silva Filho JF, Bioorganic and Medicinal Chemistry Letters . 2004,第5期

7. Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial [J] . The Lancet infectious diseases . 2016,第1期

8. THE EFFECT OF CHLOROQUINE AND RELATED ANTIMALARIALS ON HAEM IN Plasmodium falciparum [C] . J. M. Combrinck, T. E. Mabotha, K. K. Ncokazi, Annual Conference of the Microscopy Society of Southern Africa . 2012

9. Genetic Epidemiology of Plasmodium falciparum Asymptomatic Infections and Antimalarial Drug-Resistance Markers in Kilifi, Kenya [D] . Wamae, Kevin Kariuki. 2019

10. Antimalarial activity of artefenomel (OZ439) a novel synthetic antimalarial endoperoxide in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial [O] . Aung Pyae Phyo, Podjanee Jittamala, François H Nosten, -1

11. Artemisinin Derivatives with Antimalarial Activity against Plasmodium falciparum Designed with the Aid of Quantum Chemical and Partial Least Squares Methods [O] . Jose C. Pinheiro, Rudolf Kiralj, Ma¬rcia M. C. Ferreira, 2014

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2. N-2-(4,6-二取代嘧啶基)-2-(2,4-二氯苯氧基) 丙酰胺衍生物的合成与生物活性研究 [C] . 薛允宁 ,刘国华 ,薛思佳 . 中国化工学会农药专业委员会第十二届年会 . 2005

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