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Nitazoxanide derivative and medical application thereof

A technology of nitazoxanide and derivatives is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, applications, etc., and can solve problems such as restricting new medicinal uses and the like

Pending Publication Date: 2021-03-12
BEIJING MEIBEITA DRUG RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Therefore, how to improve the curative effect of old drugs has become a bottleneck restricting their new medicinal uses.

Method used

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  • Nitazoxanide derivative and medical application thereof
  • Nitazoxanide derivative and medical application thereof
  • Nitazoxanide derivative and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of o-N-(5-nitrothiazol-2-yl)carbamoyl-phenol-pyridine-3-carboxylate (I-1)

[0029]

Embodiment 11

[0030] Embodiment 1.1 The synthesis of deacetyl nitazoxanide

[0031] Take 30.00 g of nitazoxanide, add it to a 250 ml single-necked bottle, add 180 ml of concentrated hydrochloric acid, stir and disperse at room temperature; heat the system to 50°C and stir for about 15 hours. After completion of the reaction, the reaction system was cooled to room temperature, filtered, and the filter cake was washed with 50 ml × 3 times of purified water. After pumping to dryness, the filter cake was air-dried at 60° C. for 12 hours to obtain 21.1 g of deacetyl nitazoxanide as a pale yellow solid.

Embodiment 12

[0032] Example 1.2 Synthesis of o-N-(5-nitrothiazol-2-yl)carbamoyl-phenol-pyridine-3-carboxylate (I-1)

[0033] Under the protection of argon, add 3.0 g of deacetyl nitazoxanide to 75 ml of tetrahydrofuran solvent, add 5.6 g of triethylamine under stirring, stir and dissolve until clear; cool in an ice bath to 0°C, add 5.8 g of it in batches under stirring Pyridine-3-formyl chloride hydrochloride, after the addition was completed, it was stirred for 0.5 hours under the condition of ice bath and under the protection of argon, and then left at room temperature for 15 hours to react. The insolubles were removed by filtration, the filter cake was washed with 5ml of tetrahydrofuran, and the washed filtrates were combined and evaporated to dryness under reduced pressure. The residue was separated by silica gel column chromatography and eluted with dichloromethane / methanol (10 / 1). The desired components were collected and evaporated to dryness under reduced pressure to obtain 2.3 g o...

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Abstract

The invention relates to a novel nitazoxanide derivative represented by a formula I, wherein in the formula I, R is H, CH3, Cl or F and is connected to any position of a benzene ring, and X is NO2, Clor Br.

Description

technical field [0001] The present invention relates to novel nitazoxanide derivatives and non-toxic pharmaceutically acceptable salts and hydrates thereof. Background technique [0002] Nitazoxanide (chemical name: o-N-(5-nitrothiazol-2-yl)carbamoyl-phenol-acetate) is a nitrothiazole salicylic acid amide with antiprotozoal, anti-intestinal It has antiparasitic and antibacterial effects, and its antiparasitic spectrum and antibacterial spectrum are wider than albendazole and metronidazole. [0003] [0004] Further studies have found that nitazoxanide and its analogues such as RM-5038 also have broad-spectrum antiviral activity, and have inhibitory effects on various respiratory viruses, hepatitis C virus and hepatitis B virus. [0005] Nitazoxanide also has good antitumor activity. Recent research results show that nitazoxanide also has a certain hypoglycemic effect. These research results bring the prospect of new use of old drugs for nitazoxanide. [0006] But like...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/4439A61P31/20A61P3/10A61P1/16
CPCC07D417/12A61P31/20A61P3/10A61P1/16A61K31/4439A61K31/425A61K31/426A01N43/78A61K31/428
Inventor 仲伯华王晓再李宏武张小波杨家俊
Owner BEIJING MEIBEITA DRUG RES
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