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Compound and application of compound in preparation of drugs for resisting parasitic diseases

A compound and reaction technology, applied in the field of application in the preparation of antiparasitic drugs

Active Publication Date: 2014-05-14
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] None of the existing antimalarial drugs can kill all stages of the life cycle of Plasmodium, and different antimalarial drugs act on different stages

Method used

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  • Compound and application of compound in preparation of drugs for resisting parasitic diseases
  • Compound and application of compound in preparation of drugs for resisting parasitic diseases
  • Compound and application of compound in preparation of drugs for resisting parasitic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Embodiment 1, the preparation of compound

[0091] 1. Intermediate A 1 preparation of

[0092] For the preparation flow chart, see figure 1 .

[0093] Add p-3g p-bromoacetophenone, 570mg cuprous iodide, 738mg 2-pyridinecarboxylic acid, 6.4g potassium phosphate, 3.9ml p-trifluoromethoxyphenol and 15ml dimethyl sulfoxide in a round bottom flask, under argon Heating and stirring at 110°C for 20 hours under gas-protected conditions, then cooling to room temperature, adding 100ml of water to dilute, then extracting with dichloromethane 3 times (adding 25ml of dichloromethane each time), combining the organic phases extracted three times, washing with water After two times, dry with anhydrous sodium sulfate, then spin dry the solvent under reduced pressure, and pass the residue through a silica gel column with petroleum ether: ethyl acetate = 25:1 (volume ratio) to obtain 3.7g of intermediate A 1 (Intermediate A 1 As light yellow liquid), the yield was 84%.

[0094] 2. ...

Embodiment 2

[0163] Example 2, the inhibitory effect of the compound on the activity of NDH-2 protein

[0164] 1. Experimental principle

[0165] The chemical reaction catalyzed by NDH-2 (type II NADH dehydrogenase) is: NADH+UQ→NAD + +UQH 2 ; Among them, NADH has light absorption at 340nm, so the reduction rate of NADH can be evaluated by the decrease of light absorption value at 340nm.

[0166] 2. Preparation of experimental materials

[0167] (1) Preparation of NDH-2 protein

[0168] Express the NDH-2 protein of Plasmodium falciparum 3D7 strain in Escherichia coli (the NDH-2 protein is made up of 533 amino acid residues, as shown in sequence 1 of the sequence table, the 1st to 24th amino acid residues from the N-terminal are signals The peptide is used to locate the protein on the inner mitochondrial membrane of Plasmodium; the NDH-2 gene consists of 1602 nucleotides, as shown in sequence 2 of the sequence table), and the specific steps are as follows:

[0169] 1. Synthesize the dou...

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Abstract

The invention discloses a compound and application of the compound in preparation of drugs for resisting parasitic diseases. The compound has the chemical formula (VII), in the chemical formula (VII), L is O or CH2, one of R1 and R2 is a halogen element, and the other is H. The compound provided by the invention belongs to a quinolones compound; through research, an inventor finds that the compound can inhibit activity of NDH-2 protein of plasmodium, and therefore, the compound can be used for slowing down the clinical symptoms at asexual reproduction stage and also can be used for stopping diseases spreading at the sexual reproduction stage of life cycle of plasmodium. The compound has great significances for treating the plasmodium diseases. The chemical formula (VII) is as shown in the specification.

Description

technical field [0001] The invention relates to a compound and its application in preparing antiparasitic medicine. Background technique [0002] Malaria is a global acute infectious disease caused by Plasmodium falciparum and transmitted by Anopheles mosquitoes. It is the most harmful parasitic disease to humans. The pathogenic Plasmodium mainly includes Plasmodium vivax, Plasmodium malariae, Plasmodium ovale and Plasmodium falciparum, which cause Plasmodium vivax, Plasmodium malariae, Plasmodium ovale and Plasmodium falciparum respectively. , falciparum malaria infection is the most widespread, the symptoms are severe, and it is the most harmful to human health. Worldwide, there are as many as 300 million malaria patients each year, causing millions of deaths. [0003] None of the existing antimalarial drugs can kill all stages of the life cycle of Plasmodium, and different antimalarial drugs act on different stages. [0004] Plasmodium falciparum type II reduced coenzy...

Claims

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Application Information

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IPC IPC(8): C07D215/233A61K31/47A61P33/06
CPCC07D215/233Y02A50/30
Inventor 饶燏杨茂君杨毅庆冯越
Owner TSINGHUA UNIV
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