Compound for preventing and treating bacterial infection and its prepn and use

A compound and bacterial technology, applied in the field of a class of compounds for treating or preventing bacterial infections and their preparation and use, can solve problems such as drug resistance

Inactive Publication Date: 2006-08-02
SHANGHAI DONGHAO MEDICINE BIOLOGY ENTERPRISE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this development method has achieved some success, the new variants usually show better efficacy than the old drugs, have a broader antibacterial spectrum, or can overcome some drug resistance mechanisms, but shortly after the market, microorganisms are resistant to various new drugs. resistance

Method used

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  • Compound for preventing and treating bacterial infection and its prepn and use
  • Compound for preventing and treating bacterial infection and its prepn and use
  • Compound for preventing and treating bacterial infection and its prepn and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Embodiment 1. the synthesis of novel antibacterial compound series

[0099]Infectious diseases are currently one of the main factors leading to the death of the world's population. According to the statistics of the World Health Organization in 2002, in the past 10 years, the number of deaths due to infectious diseases has exceeded a quarter of the world's annual death toll. There was once optimism that infectious diseases had been conquered because of the discovery of antibiotics. However, the ensuing problem of bacterial resistance has awakened human beings from their dreams. Half a century ago, most infections caused by Staphylococcus aureus were sensitive to penicillin. Today, such infections are not only resistant to penicillin, but also to many antibiotics developed later. In addition to hospital-acquired infections, the problem of bacterial resistance is threatening healthy populations. Diseases that were once manageable (such as gonorrhea, typhoid, and tuberc...

Embodiment 2

[0136] Example 2. Activity of Novel Antibacterial Compounds

[0137] The compounds EB-1 and EB-2 described here should be 4-(4-biphenyl)-4'-guanidinium methylbenzoate hydrochloride and 4-(4-aminobiphenyl) respectively -4'-guanidine methylbenzamide hydrochloride can specifically inhibit the growth of cocci. 8 synthetic compounds were tested against Staphylococcus aureus standard strain (ATCC25923), Sarcina luteus standard strain (ATCC9341), Staphylococcus epidermidis standard strain (ATCC12228), Pseudomonas aeruginosa standard strain (ATCC2785), Shigella standard strain (Shanghai Health and Epidemic Prevention Station 51573) and Escherichia coli standard strain (ATCC25922) the minimum inhibitory concentration (MIC, μg / ml), EB-1 and EB-2 against cocci MIC range from 1.25 to 10μg / ml. Compared with the broad-spectrum antibiotic ceftriaxone, the above compounds have no obvious inhibitory activity on rod-shaped bacteria (see Table 1).

[0138] Table 1

[0139] In order to know ...

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PUM

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Abstract

The present invention relates to compound for preventing and treating bacterial infection, especially diseases caused by methicillin resisting Staphylococcus aureus, methicillin resisting Staphylococcus epidermidis, Escherichia coli producing extremely-broad spectrum beta-lactamases, Klebsiella pneumoniae and fecal enterococcus producing inactivating enzyme, and its preparation process and medical use.

Description

technical field [0001] The present invention relates to the treatment or prevention of infection by certain bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphylococcus epidermidis (MRSE), extended-spectrum beta-lactamases (ESBLs) ) of Escherichia coli and Klebsiella pneumoniae and inactivated enzyme-producing Enterococcus faecalis infection caused or accompanying diseases or symptoms, its preparation method and medical use. Background technique [0002] The 20th century was an era of rapid development of antibacterial drugs. In the 1930s, sulfa drugs were discovered, and penicillin was initially used in the 1940s. A large number of important antibiotics such as aminoglycosides, chloramphenicol, tetracyclines, and macrolides were developed immediately, followed by semi-synthetic penicillins, cephalosporins, and new β-lactams. The advent of antibacterial drugs such as quinolones and quinolones has made effective treatment of v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/14A61K31/165A61P31/04A61P11/00A61P13/02A61P1/16A61P15/00A61P17/00A61P1/02
CPCY02A50/30
Inventor 王明伟谢建树朱德煦村松睦唐磊李伯俊
Owner SHANGHAI DONGHAO MEDICINE BIOLOGY ENTERPRISE
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