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Application of N-(2-thiazole)benzamide derivatives

A technology of benzamide and thiazole, applied to N-benzamide derivatives in the field of medicine

Inactive Publication Date: 2013-09-11
SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although existing studies have proved that nitazoxanide can be used for the treatment of gastroenteritis, hepatitis C, and hepatitis B caused by rotavirus and norovirus (Norovirus), nitazoxanide has not been used in the treatment of Japanese encephalitis virus infection. see any reports

Method used

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  • Application of N-(2-thiazole)benzamide derivatives
  • Application of N-(2-thiazole)benzamide derivatives
  • Application of N-(2-thiazole)benzamide derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1 Nitazoxanide inhibits Japanese encephalitis virus proliferation in BHK cells (golden hamster kidney cells) in vitro

[0084] Implementation steps:

[0085] (1) Cell culture

[0086] BHK cells in good growth state were subcultured on a 6-well cell culture plate (Corning, USA) (1×10 6 cells / well). After 12 hours, wash with serum-free DMEM (GIBCO product in the United States) medium, and add 1 × 10 cells to each well. 3 TCID 50 The Japanese encephalitis virus was placed in a cell culture incubator at 37°C for 1 hour. After taking it out, wash it twice with serum-free DMEM, and then add cell culture medium containing 5 μg / ml nitazoxanide (containing 2% calf serum, 100 units of penicillin and 100 units of streptomycin). At the same time, the following control groups were set up: a. virus inoculation plus nitazoxanide group; b. virus inoculation plus dimethyl sulfoxide group.

[0087] (2) Sample collection

[0088] At the moment of 0h, 6h, 12h, 18h and 24h...

Embodiment 2

[0105] Example 2 The inhibitory effect of nitazoxanide derivatives of the present invention on the proliferation of Japanese encephalitis virus in BHK cells in vitro

[0106] The specific implementation steps are the same as in Example 1, and the specific test data are shown in Tables 3 to 12, and the curves are drawn according to Tables 3 to 12 Figure 2-11 .

[0107] according to Figure 2-11 It can be seen that the nitazoxanide derivatives Tizoxanide, RM4803, RM4832, RM4848, RM4850, RM4851, RM4852, RM4863, RM4865 and RM5014 of the present invention can effectively inhibit the proliferation of Japanese encephalitis virus in BHK cells.

[0108] Table 3: Titers of Japanese encephalitis virus in BHK cells after Tizoxanide treatment

[0109]

[0110] Table 4: JE virus titers in BHK cells after RM4803 treatment

[0111]

[0112] Table 5: JE virus titers in BHK cells after RM4832 treatment

[0113]

[0114] Table 6: JE virus titers in BHK cells after RM4848 treatment ...

Embodiment 3

[0129] Embodiment 3 Nitazoxanide inhibits Japanese encephalitis virus proliferation in mice

[0130] Implementation steps:

[0131] (1) Animals: 40 female Kunming mice (Shanghai Slack Experimental Animal Co., Ltd.), weighing 12-14 g. Divided into 4 groups on average:

[0132] a. Add dimethyl sulfoxide to the drinking water of the poisoned mice;

[0133] b. Nitazoxanide was added to the drinking water of the poisoned mice;

[0134] c. Nitazoxanide was added to the drinking water of uninfected mice;

[0135] d. The drinking water of uninfected mice was normal.

[0136] (2) Nitazoxanide treatment test on JEV-infected Kunming mice: treat the mice according to the grouping method in (1), and inject 100 ID into the Kunming mice intraperitoneally 50 Japanese encephalitis virus. After 1 day, for the mice in group b (infected mice drinking water plus nitazoxanide group), add a dimethyl sulfoxide solution of nitazoxanide (concentration is 100 μg / ml) in its drinking water to ensure t...

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Abstract

The invention discloses an application of N-(2-thiazole)benzamide compounds represented by a formula A in preparations of medicines used for resisting Japanese encephalitis virus infection, wherein R1 is OH, OCOCH3, OCOC2H5, OCOCH2CH2CH3 or OCOCH(CH3)2; R2, R3 and R4 are independently H or C1-C3 alkyl; R5 is halogen, nitro or C1-C3 alkylsulfuryl; and R6 is H or C1-C3 alkylsulfuryl. The invention also relates to an application of the compounds A in preparations of medicines used for preventing and / or treating Japanese encephalitis virus infection. With the N-(2-thiazole)benzamide compounds provided by the invention, reduplication of Japanese encephalitis virus can be effectively inhibited. The formula A is presented below.

Description

technical field [0001] The invention relates to the application of a class of N-(2-thiazole) benzamide derivatives in the field of medicine. Background technique [0002] Japanese Encephalitis (JE), also known as JE, is a viral encephalitis caused by Japanese encephalitis virus (JEV) infection. The disease is mainly transmitted by the bite of Culex mosquitoes. JE virus infection can cause severe neurological disorders and meningitis, and about 1-3 of every 1,000 JE virus-infected patients are accompanied by neurological diseases, and the fatality rate of JE virus is about 30%. [0003] Every year, there are about 30,000-50,000 Japanese encephalitis clinical patients worldwide, and more than 10,000 deaths, and they are mainly distributed in China, Southeast Asia, India and other countries. At present, the epidemic range of Japanese encephalitis has expanded to South Asia, East Asia, Southeast Asia and the Asia Pacific Rim region. About 3 billion people in the world live in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/426A61K31/625A61P31/14
CPCY02A50/30
Inventor 马志永史子学邱亚峰沈阳邵东华薛飞群
Owner SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI