N-acylhydrazone-ciprofloxacin heterozygote and preparation method and application thereof
A technology of ciprofloxacin and acyl hydrazone, which is applied in the field of antibacterial and can solve the problems of increasing bacterial resistance and the like
Active Publication Date: 2021-02-12
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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Abstract
The invention discloses an N-acylhydrazone-ciprofloxacin heterozygote and a preparation method and application thereof. The structural formula of the N-acylhydrazone-ciprofloxacin heterozygote is shown as a formula (II). A series of N-acylhydrazone-ciprofloxacin heterozygotes with brand-new structures are designed and synthesized by introducing an antibacterial pharmacophore N-acylhydrazone to thenitrogen atom of a ciprofloxacin C-7 piperazinyl, and the preparation method comprises the following steps: taking ethyl chloroacetate or ethyl bromoacetate and ciprofloxacin as raw materials, carrying out substitution reaction to obtain a precursor compound; reacting the precursor compound with hydrazine hydrate under a heating condition to obtain an N-hydrazide-ciprofloxacin intermediate (I), and reacting the intermediate (I) with aldehyde to obtain the N-acylhydrazone ciprofloxacin heterozygote (II). The heterozygote shows antibacterial activity, particularly has good antibacterial activity on staphylococcus aureus, escherichia coli and pseudomonas aeruginosa, and can be used as an antibacterial candidate compound.
Application Domain
Antibacterial agentsOrganic chemistry +1
Technology Topic
PiperazinePharmacophore +19
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