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ALD and application thereof as EV71 virus and CAV16 virus inhibitor

A technology of CAV16 and EV71, applied in the field of ALD and its use as an inhibitor of EV71 virus and CAV16 virus, can solve the problems such as the listing of specific antiviral drugs for hand, foot and mouth disease

Active Publication Date: 2015-07-01
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no specific antiviral drug for hand, foot and mouth disease on the market

Method used

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  • ALD and application thereof as EV71 virus and CAV16 virus inhibitor
  • ALD and application thereof as EV71 virus and CAV16 virus inhibitor
  • ALD and application thereof as EV71 virus and CAV16 virus inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: R is -CH 3 Synthesis of the compound of the present invention:

[0028] (1) Add 4-bromopyridin-2-amine (5g, 28.90mmol), di-tert-butyl carbonate ((Boc) 2 O) (6.8g, 31.16mmol), 4-dimethylaminopyridine (0.32g), tert-Butanol (70mL). Stir overnight at room temperature and concentrate in vacuo. The resulting mixture was washed with 30 ml of n-hexane / ether (hexane / ether) with a volume ratio of 5:1 to obtain N-tert-butoxycarbonyl-4-bromo-pyridine-2-amine (tert-butyl N-(4-bromopyridin-2-yl)carbamate) (4.5g, 57%), a white solid.

[0029] (2) Under nitrogen, add tert-butyl-N-(4-bromopyridin-2-yl) carbonate (that is, the N-tert-butoxycarbonyl-4-prepared in step (1)) into a 50 ml round bottom flask. Bromo-pyridine-2-amine) (820mg, 3.00mmol), 1-(5-[4-[(ethoxyimine)methyl]phenoxy]-3-methylpentyl)-imidazoline- 2-ketone (1-(5-[4-[(ethoxyimino)methyl]phenoxy]-3-methylpentyl)imidazolidin-2-one) (500mg, 1.50mmol), Johnphos (2-(di-tert-butylphosphine) Benzene) (45mg), Pd(dba) 2 (38...

Embodiment 2

[0065] Example 2: The inhibitor compound prepared in Example 1 inhibits the activity of five hand-foot-mouth disease-causing viruses EV71(A), EV71(B), EV71(C), CAV16(A) and CAV16(B) infecting cells Determination

[0066] The inhibitor compound prepared in Example 1 was dissolved in 95% DMSO, prepared as a solution with a concentration of 10 mM, and stored at 4°C for later use.

[0067] According to experimental step 6 (inhibitor inhibits virus infection IC 50 The contents described in the determination of the value) were performed to test the protective effects of the inhibitor compound on the two types of cells (RD cells and Vero cells) under the above five virus infections. According to the method in experiment step 5, observe the corresponding inhibitor concentration when half of the cells have lesions, and obtain the IC50 value. The final measured results are shown in Table 2:

[0068] Table 2

[0069]

[0070]

[0071] It can be seen from the above experiments that the compound...

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PUM

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Abstract

The invention discloses an ALD derivative or pharmaceutically acceptable salts thereof, and further provides application of the ALD derivative or the pharmaceutically acceptable salts thereof as EV71 virus and CAV16 virus inhibitors and application of the ALD derivative or the pharmaceutically acceptable salts thereof in preparing medicines for treating hand-foot-and-mouth diseases. The structural formula of the ALD derivative is as shown in the specification. The invention further provides a method for preparing the ALD derivative or the pharmaceutically acceptable salts thereof.

Description

Technical field [0001] The present invention relates to ALD derivatives and their pharmaceutically acceptable salts and their applications in the preparation of medicines, in particular to the use of ALD derivatives and their pharmaceutically acceptable salts in inhibiting EV71 virus and CAV16 virus . Background technique [0002] Hand-foot-mouth disease (Hand-foot-mouth disease, HFMD) is a common global infectious disease. my country has always been an area with a high incidence of hand-foot-mouth disease. The number of new cases of hand-foot-mouth disease in China continued in 2010, 2011, and 2012. In the past three years, it has ranked first among legal infectious diseases in my country, and there is a clear upward trend. There is no specific antiviral drug for hand, foot and mouth disease currently on the market. [0003] Human enterovirus 71 (EV71 virus) and Coxsackie A16 virus (CAV16 virus) are the main pathogens causing hand, foot and mouth disease in my country in recent y...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/4439A61P31/14
CPCC07D401/04
Inventor 饶子和王祥喜彭伟李雪梅杨诚陈卫强李爽大卫·斯图尔德
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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