Compounds for inhibiting multi-medicine medicine-resistant staphylococcus aureus activity

Abstract

The invention belongs to the pharmaceutical field, and relates to compound of 1S<*>,2R<*>,7R<*>-3-benzoyl-2-hydroxy-8,8-dimethyl-1,5,7-tri(3-methyl-2-butenyl)-bbicyclo-[3.3.1]nonan-2-ene-4,9-dione. The compound has the molecular formula and the plane structure of 7-epiclusianone. The stereochemical configuration of a chiral carbon atom is the enantiomer of 7-epiclusianone, and is named as ent-7-epiclusianone. The pharmacological and bacteriostatic experimental results show that the compound has pharmacological activities for inhibiting multi-drug resistant Staphylococcus aureus; and for methi-cillin-resistant Staphylococcus aureus containing fluoroquinolone-resistant genes NorA, the minimum inhibitory concentration (MIC) of the compound is only of 4 Mu g / mL (7.3 Mu M) and the compound activity is higher than a contrast drug when the MIC of norfloxacin positive contrast drug is of 32 Mu g / mL (100 Mu M). The compound can be used for preparing antibacterial injections and external pharmaceutical preparations.

Description

A compound that inhibits the activity of multidrug-resistant staphylococcus aureus technical field The invention belongs to the field of pharmacy and relates to compound 1S*, 2R*, 7R*-3-benzoyl-2-hydroxyl-8,8-dimethyl-1,5,7-tri(3-methyl-2- Butenyl)-bicyclo[3.3.1]non-2-ene-4,9-dione, named after ent-7-epiclusianone (hereinafter referred to as HSRO1-1), and its use in the preparation of anti-fluoronoquinones Use in medicines for methicillin-resistant Staphylococcus aureus (MRSA). Background technique Antimicrobial resistance is a growing problem. Methicillin-resistant Staphylococcus aureus (MRSA) has become a common and serious infectious bacteria in hospitals in recent years. In addition to superficial skin infections, it also has deep infections inside the human body, which can lead to death in severe cases. Due to the widespread use and even abuse of antibiotics in my country in the past one or two years, especially after vancomycin has become a routine antibiotic drug...

AI Technical Summary

Problems solved by technology

In these external pump mechanisms, bacterial cells "pump out" most types of antibiotic drug molecules commonly used, so that the concentration of the drug in the cell is reduced and the antibacterial effect cannot be exerted

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