首页> 外国专利> A METHOD OF SYNTHESIS OF NIL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM

A METHOD OF SYNTHESIS OF NIL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM

机译:合成至少一种抗疟疾疟原虫恶性疟原虫抗氯喹菌株的具有高生物活性的Nil2复合物的方法

摘要

Metal complex of Nickel (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (1.4). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
机译:合成了含二硫基配体的镍(II)金属配合物,并通过元素分析,质谱,质子NMR和FT-IR光谱对其进行了表征。镉配合物的单晶X射线结构已被分析。对该金属配合物进行了来自疟疾寄生虫恶性疟原虫的falcipain-2(FP-2)和falcipain-3(FP-3)半胱氨酸蛋白酶的生物学测试。他们在体外进一步测试了抗氯喹菌株(W2)。尽管金属配合物的效力比FP-2和FP-3的对照弱,但在以强度比对耐氯喹的菌株(W2)进行测试时,发现金属配合物的效力大大高于对照。 (1.4)。本文描述了所述金属配合物的合成,表征和生物学结果,所述金属配合物具有去质子化的3- [1-(2-吡啶基)亚乙基]肼碳二硫代酸酯配体(图1)。

著录项

  • 公开/公告号IN2011MN01259A

    专利类型

  • 公开/公告日2012-08-17

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN1259/MUMNP/2011

  • 发明设计人 ENOS KIREMIRE;

    申请日2011-06-16

  • 分类号C07D213/53;

  • 国家 IN

  • 入库时间 2022-08-21 17:24:05

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