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A New Antibacterial Compound Containing Fluorine

A compound and hydrate technology, applied in antibacterial drugs, medical preparations containing active ingredients, organic chemistry, etc.

Inactive Publication Date: 2011-12-07
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs have produced different degrees of drug resistance after a period of clinical use, so it is necessary to explore new antibiotics for drug-resistant bacteria

Method used

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  • A New Antibacterial Compound Containing Fluorine
  • A New Antibacterial Compound Containing Fluorine
  • A New Antibacterial Compound Containing Fluorine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Embodiment 1: the preparation of formula 1 compound

[0011] 1. Synthesis of Compound 2a, 2b

[0012] Accurately weigh 4.26 grams of raw material a and dissolve in 20.0 mL of THF, add .4 grams of anhydrous Lithium chloride, add 1.0 g of sodium borohydride in batches at 0°C, then move the reaction solution to an oil bath to reflux for 3 hours, stop heating, cool to room temperature, add 20.0 mL of saturated The ammonium solution was separated, the organic layer was separated, the solvent was distilled off under reduced pressure, and 3.5 g of a crude product of compound 2a was obtained after vacuum drying, with a yield of 95%. The crude product was directly used in the next step without purification. MS (m / z): 185.05.

[0013] Using the same method as starting material b, 4.6 g of compound 2b was obtained with a yield of 96%, MS (m / z): 240.12.

[0014] 2. Synthesis of compounds 3a and 3b

[0015] Dissolve the crude product 2a from the previous step in 20.0 mL of THF...

Embodiment 2

[0029] Embodiment 2: the antibacterial activity research of formula 1 compound

[0030] 2.1 Materials and methods

[0031] Antibacterial drug: compound 1a (compound R=-CH of formula 1 3 ) Synthesized by Guangdong Zhongke Pharmaceutical Research Co., Ltd.

[0032] Control drug: desmethylvancomycin hydrochloride was purchased from North China Pharmaceutical Group

[0033] Tested strains: 101 strains of MRSA and 105 strains of MSSA were donated by the School of Pharmacy, Sun Yat-sen University, and determined according to the NCCLS standard after identification.

[0034] Culture medium: purchased from BioMérieux, France, batch number: 811813401.

[0035] Method: adopt double agar dilution method to measure compound 1a (formula 1 compound R=-CH 3 ), and the minimum inhibitory concentration (MIC) of demethylvancomycin hydrochloride to all strains. That is, first dilute the two antibiotics to 12 concentrations with sterile phosphate buffer solution of different concentrations a...

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Abstract

A compound with remarkable antibacterial activity has the following structure: (Formula I), which has good antibacterial effect on methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA).

Description

Technical field: [0001] The invention relates to a compound for antibacterial effect, which has good antibacterial activity against MRSA and MSSA. Background technique: [0002] In recent years, with the widespread use of antibiotics (including humans and animals), the increase in the use of glucocorticoids and immunosuppressants, and the increase in elderly patients, the problem of pulmonary drug-resistant bacterial infections has become increasingly prominent. Penicillin-resistant Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), extended-spectrum beta-lactamase (ESBL)-producing Gram-negative bacteria Wait. Methicillin-resistant Staphylococcus aureus is also a difficult issue. Since the first strain of MRSA was detected for more than 40 years, MRSA infection has been on the rise all over the world. According to the National Nosocomial Infection Surveillance (NNIS) report, 182 hospitals in 1975 MRSA acco...

Claims

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Application Information

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IPC IPC(8): C07D409/12A61K31/4436A61P31/04
Inventor 王伟周亚耀刘亚楠
Owner GUANGDONG ZHONGKE DRUG R&D
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