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Compounds with antimicrobial antiviral activity

A compound and adduct technology, applied in the field of medicine, can solve problems such as increased bacterial resistance and inconvenient clinical application

Active Publication Date: 2008-04-02
吉林津升制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The emergence and application of antibiotics have played a huge role in the prevention and treatment of infectious diseases, but at the same time, the overuse of antibiotics has led to the continuous increase of bacterial resistance, as well as the limitation of absorption in the digestive tract, which has brought a lot of inconvenience to clinical application

Method used

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  • Compounds with antimicrobial antiviral activity
  • Compounds with antimicrobial antiviral activity
  • Compounds with antimicrobial antiviral activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0134] Example 1 Preparation of sodium α-hydroxy-[(5-amino-1,2,4-thiadiazol)-3-yl]formyl ethyl sulfonate and its structure confirmation

[0135] (1) Preparation of [(5-amino-1,2,4-thiadiazol)-3-yl]formyl chloride

[0136] Under cooling in an ice bath, mix 29g (0.20mol) of [(5-amino-1,2,4-thiadiazol)-3-yl] formic acid, 100ml of anhydrous acetone, 0.5ml of anhydrous pyridine, and 38g (0.2 mol), stirred at 0°C for 1h, then heated to 15-20°C, stirred for 6 hours, poured into 100ml of ice water, stirred evenly, extracted twice with 50ml of dichloromethane, combined organic layers, dried over anhydrous sodium sulfate , concentrated under reduced pressure at 40°C to 20ml to obtain [(5-amino-1,2,4-thiadiazol)-3-yl]formyl chloride solution, which was sealed for future use.

[0137] (2) Preparation of [(5-amino-1,2,4-thiadiazol)-3-yl]formylacetaldehyde

[0138] Measure 40ml of acetaldehyde in the reaction flask, and slowly add the [(5-amino-1,2,4-thiadiazol)-3-yl]formyl chloride sol...

Embodiment 2

[0142] Example 2 Preparation and Structure Confirmation of Sodium α-Hydroxy-[(2-amino-1,3-thiazol)-4-yl]formylethylsulfonate

[0143] (1) Preparation of [(2-amino-1,3-thiazol)-4-yl]formyl chloride

[0144] Under ice-bath cooling, 28.8g (0.20mol) [(2-amino-1,3-thiazol)-4-yl] formic acid was added in the reaction flask, and the operation method was then referred to step (1) in Example 1 to obtain [(2-Amino-1,3-thiazol)-3-yl]formyl chloride solution, sealed for future use.

[0145] (2) Preparation of [(2-amino-1,3-thiazol)-4-yl]formylacetaldehyde

[0146] The operation method refers to step (2) in Example 1 to obtain an aqueous solution of [(2-amino-1,3-thiazol)-4-yl]formylacetaldehyde, and directly proceed to the next reaction.

[0147] (3) Preparation of α-hydroxyl-[(2-amino-1,3-thiazol)-4-yl]sodium formyl ethyl sulfonate

[0148] The operation method refers to step (3) in Example 1 to obtain 41.8 g of sodium α-hydroxy-[(2-amino-1,3-thiazol)-4-yl]formyl ethyl sulfonate wit...

Embodiment 3

[0150] Example 3 Preparation of sodium α-hydroxy-[(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetyl ethyl sulfonate and its structure confirmation

[0151] (1) Preparation of [(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetyl chloride

[0152] Under cooling in an ice bath, add 37g (0.20mol) [(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetic acid into the reaction flask, and then refer to Example 1 for the operation method In step (1), [(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetyl chloride solution is obtained, which is sealed for future use.

[0153] (2) Preparation of [(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetoacetaldehyde

[0154] The operation method refers to step (2) in Example 1 to obtain an aqueous solution of [(2-methyl-5-nitro-1,3-oxadiazol)-1-yl]acetoacetaldehyde, and directly proceed to the next reaction.

[0155] (3) Preparation of α-hydroxy-[(2-methyl-5-nitro-1,3-oxadiazole)-1-yl] sodium acetyl ethyl sulfonate

[0156]The operation method refers to (c) in Example 2 to obta...

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Abstract

The present invention belongs to the field of medical technology and relates to a compound and adduct with antibacterial and antiviral activity. Wherein, R, n, and m are defined as in the specification. The present invention also relates to drug compositions containing the compound and adduct, and the application of the compound and adduct in preparation of drugs for treating and / or preventing infectious diseases. The compound and adduct of the present invention have broad-spectrum and high-efficiency antibacterial and antiviral activity; in vitro and in vivo, the compound and adduct have high antibacterial activity for Gram-positive and negative bacteria, aerobic and anaerobic bacteria and fungi. At the same time, the compound and adduct have high anti-virus activity and good values for clinical application.

Description

1. Technical field [0001] The present invention relates to compounds with antibacterial and antiviral activity and their adducts, pharmaceutical compositions containing these compounds or their adducts, and the use of these compounds or their adducts in the preparation of medicines for treating and / or preventing infectious diseases The application belongs to the field of medical technology. 2. Background technology [0002] Infectious diseases are diseases caused by bacteria, viruses, fungi, etc. It is one of the major clinical diseases and seriously endangers human life and health. The emergence and application of antibiotics have played a huge role in the prevention and treatment of infectious diseases, but at the same time, the overuse of antibiotics has led to the continuous increase of bacterial resistance, as well as the limitation of absorption in the digestive tract, which has brought a lot of inconvenience to clinical application. [0003] Due to the large number o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D285/08C07D277/40C07D277/56C07D233/92C07D249/10A61K31/433A61K31/426A61K31/4164A61K31/4196A61P31/00
Inventor 黄振华
Owner 吉林津升制药有限公司
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