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Diaromatic compound with bioactivity

A compound and aromatic technology, applied in the field of aromatic compounds, can solve the problem of high price

Inactive Publication Date: 2013-03-13
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of hepatitis B is still a worldwide medical problem. Although drugs for hepatitis B such as interferon, lamivudine, and entecavir have been developed at home and abroad, these drugs are expensive and not 100% effective

Method used

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  • Diaromatic compound with bioactivity
  • Diaromatic compound with bioactivity
  • Diaromatic compound with bioactivity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of biaromatic compound:

[0032] The biaromatic compounds involved in the present invention can be prepared according to the following two methods, wherein method one is used to prepare new chiral biaromatic compounds, and method two is used to prepare racemic new biaromatic compounds.

[0033] Method 1: At room temperature to 80℃, the substrate concentration is 0.04~2.0mol / L, and Zn is neutralized in 0.1~1 equivalent of tetraalkylammonium halide (such as tetra-n-butylammonium iodide) in a polar organic solvent In the presence of a chiral monophosphine ligand and a divalent or zero-valent nickel complex catalyst catalyzed, the moles of substrate and catalyst are 10-100:1, react for 3 to 6 hours, and then purified by column chromatography. The product is obtained with a certain yield and certain optical purity; the general reaction formula is as follows:

[0034]

[0035] Among them, the main configuration of the product is determined by the configuration...

Embodiment 2

[0044] Example 2 Biological experiment:

[0045] Test materials and methods

[0046] 1. The sample is dissolved in DMSO to prepare 20mg / mL, and then diluted with DMEM culture solution to different concentrations.

[0047] 2. Cell model: hepatitis B virus (HBV) transfection of HepG 2 Cell, namely HepG 2 2.2.15 cells.

[0048] 3. Drug toxicity test: MTT method MTT (Aldrich)

[0049] 4. HBV antigen detection: ELISA method Shanghai Industrial Kehua Biotechnology Co., Ltd. kit

[0050] 5. Drug toxicity test:

[0051] Add 120μl (4×10 5 cells / mL)Hep G 2 .2.2.15 cells, 37°C, 5% CO 2 The monolayer was cultured for 72 hours, the supernatant was discarded, and the medicinal solution prepared to 5 concentrations as required was added, and a cell control group was set up. Change the sample solution every 3 days for 9 days in total, discard the supernatant, add 90μL ofDMEM and 10μL ofthe 5mg / ml MTT in the incubator for 3hours. Discard the supernatant, add 100μl of DMSO, culture plate at 50rpm Shake f...

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Abstract

The invention provides a diaromatic compound, having the structure formula on the right. The diaromatic compound is screened through an inhibiting test on HBVs antigen and e antigen excrete by a cell model, hepatitis B virus (HBV) transfect HepG2 cell (namely a HepG[2]2.2.15 cell), and most compounds are found to have certain inhibiting action, wherein several specific compounds show good activity with the highest inhibition ratio reaching 58.5 percent, and show stable treating effect in multiple rounds of tests. Based on the effect, the 3-substituted phthalide is a molecule with anti HBV bioactivity, and can be used for preparing medicines.

Description

Technical field [0001] The present invention relates to a series of biaromatic compounds with biological activity. Background technique [0002] Viral hepatitis B is an infectious disease caused by hepatitis B virus (HBV) that causes liver damage, which seriously harms health and affects the quality of life. HBV infection has a global distribution. It is possible that more than half of the world's population has been infected. There are 50 million new infections every year and one million deaths every year. About 5% of the world's population are carriers of chronic hepatitis B surface antigen (HBsAg). The incidence is high in developing countries. my country is the country with the most serious hepatitis B infection in the world and belongs to a high endemic area. In 2003, my country reported 710,000 cases of hepatitis B, accounting for 28% of the total number of legally reported infectious diseases that year. About 120 million people in my country were long-term carriers of h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C47/575C07C69/16C07D317/64C07C205/44C07C45/72C07C67/343C07C201/12A61K31/11A61K31/222A61K31/36A61P31/14
Inventor 林国强徐明华陈雯雯赵骞周珮史训龙
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI