Applications of H2dpa and derivatives thereof as metal beta-lactamase inhibitor in antibiosis
The invention belongs to the technical field of medicinal chemistry, and relates to applications of a metal beta-lactamase inhibitor H2dpa and derivatives thereof in the antibacterial field. The compounds have the following structures. Through experiments, the compounds 1, 2, 3 and 4 all have better...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention belongs to the technical field of medicinal chemistry, and relates to applications of a metal beta-lactamase inhibitor H2dpa and derivatives thereof in the antibacterial field. The compounds have the following structures. Through experiments, the compounds 1, 2, 3 and 4 all have better inhibitory activity on metal beta-lactamase (NDM-1, IMP-4 and VIM-1), and can recover the antibacterial activity of engineering strains for producing the metal beta-lactamase and clinically separated enterobacteriaceae bacteria on carbapenem antibiotics. The MIC value of carbapenem drug-resistant escherichia coli (NDM-1-producing metal beta-lactamase) to meropenem can be reduced by at least 2048 times at most. The compound 3 and the meropenem are combined for use, so that strains capable of producing MBL can be quickly killed. A toxicity experiment proves that the compound has very small in-vitro cytotoxicity and in-vivo toxicity. A mouse in-vivo experiment shows that the survival rate of a mouse infected with MBL |
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