Application of aromatic nitro compound in preparing medicine for treating virus hepatitis

A technology of viral hepatitis and aromatic nitro, which is applied in the direction of antiviral agents, drug combinations, digestive system, etc., can solve the problems of unreported application and achieve the effect of inhibiting proliferation

Inactive Publication Date: 2008-06-04
上海富海科星咨询管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] 4-iodo-3-nitrobenzamide belongs to the nucleocapsid protein p7 inhibitor of aromatic nitro compounds. The structural formula is shown in the figure below. It has anti-HIV virus activity, but its application in the field of hepatitis treatment has not yet been report

Method used

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  • Application of aromatic nitro compound in preparing medicine for treating virus hepatitis
  • Application of aromatic nitro compound in preparing medicine for treating virus hepatitis
  • Application of aromatic nitro compound in preparing medicine for treating virus hepatitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Synthesis of nitroaromatic compounds

[0030] Preparation of 4-iodo-3-nitrobenzamide

[0031]1025mg of 4-iodo-3-nitrobenzoic acid (provided by Chemica Alta Ltd., Edmonton, Alberta, Canada) was dissolved in 10ml of N,N-dimethylformamide, cooled to 10°C, then 0.76ml of chlorinated Sulfoxide, stirred at room temperature for 1 hour, then added to 20ml of pre-cooled concentrated ammonia water to obtain a black-yellow mixture, stirred for 5 minutes, added 50ml of pre-cooled deionized water, a bright yellow precipitate appeared, and cooled in an ice bath for 10 minutes , the precipitate was filtered off with suction, rinsed with cold water and then dried in vacuo to obtain 500.4 mg of crude product, which was recrystallized from acetonitrile to obtain 415.2 mg of 4-iodo-3-nitrobenzamide, melting point: 152-155°C. HNMR (DMSO) δ 7.67 (bs, 1H, a non-equivalent proton in the amide group), 7.84, 7.85 and 7.86, 7.87 (dd, 1H, the 5th hydrogen of the aromatic ring), 8.22 an...

Embodiment 2

[0032] Example 2: In vitro experimental study of anti-hepatitis B

[0033] Material

[0034] 4-iodo-3-nitrobenzamide was prepared with DMSO to make an appropriate concentration in the experiment, and the culture medium was diluted 3 times during the test, with a total of 8 dilutions.

[0035] Positive control drug: Lamivudine was produced by Glaxo Wellcome.

[0036] method

[0037] Drug-to-cytotoxicity test HepG2.2.15 cells were dispersed into a single cell suspension with 0.6% trypsin, and the concentration was 3 × 10 in DMEM medium containing 10% fetal bovine serum. 5 Cell suspension of cells / ml, seeded at 0.1ml / well in a 96-well plate, placed at 37°C, saturated humidity, 5% CO 2 Culture in an incubator, and change 0.1 ml / well of drug-containing culture medium after 2 days, with four wells for each concentration. The drug stock solution was serially diluted to 8 concentrations. Set to 37℃, saturated humidity, 5%CO 2 The culture was continued in the incubator, and a con...

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PUM

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Abstract

The invention relates to a novel application of aromatic nitro compound in the pharmaceutical field, in particular to the application of aromatic nitro compound in treating viral hepatitis. The aromatic nitro compound can be used alone or can be combined with other commonly used anti- viral hepatitis drugs to effectively restrain the replication and secretion of hepatitis virus. The aromatic nitro compound can remarkably restrain the replication and secretion of hepatitis virus in the bodies of mammals. The aromatic nitro compound is especially suitable for treating the diseases caused by hepatitis B virus and hepatitis C. The invention provides the concrete method for treating the patients with hepatitis B and hepatitis C.

Description

technical field [0001] The present invention relates to the field of treatment of viral hepatitis, more particularly, the present invention relates to the application of 3-nitro-4-iodo-benzamide and its derivatives alone or in combination with other antiviral compounds in the treatment of viral hepatitis. Background technique [0002] Viral hepatitis (viral heptitis) is a common infectious disease caused by a variety of hepatitis viruses. The main clinical manifestations are fatigue, loss of appetite, nausea, vomiting, hepatomegaly and liver function damage. Some patients may have jaundice and fever. Some patients experience hives, arthralgia, or upper respiratory symptoms. There are five types of viral hepatitis: A, B, C, D and E. In the past, the so-called non-A non-B hepatitis (NANBH) was infected through blood, called post-transfusion non-A non-B hepatitis (PT-NANBH), and the fecal-oral infection was called enteric-transmitted non-A non-B hepatitis ( ET-NANBH), in rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/166A61P31/12A61P1/16
Inventor 劳苑子万维勤赵新永章承继陈车生
Owner 上海富海科星咨询管理有限公司
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