Compound for recovering sensitivity of beta-lactam antibiotics, composition and application

By developing a novel boric acid compound, the problem of MRSA resistance to β-lactam antibiotics was solved, the metabolic stability and biological activity of the compound were improved, the sensitivity of bacteria to antibiotics was restored, and the therapeutic effect was enhanced.

CN121949355APending Publication Date: 2026-05-01JIANGNAN UNIV
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Patent Information

Application Number
CN202411528485.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-10-30
Publication Date
2026-05-01

AI Technical Summary

Technical Problem

The resistance of existing β-lactam antibiotics to Staphylococcus aureus, especially MRSA, leads to decreased treatment efficacy, and existing compounds have insufficient metabolic stability and biological activity.

Method used

To develop a novel boric acid compound and its pharmaceutically acceptable salt to restore bacterial sensitivity to β-lactam antibiotics by interfering with the β-lactam antibiotic response pathway. This includes boric acid compounds with different structures and their pharmaceutically acceptable salts, hydrates, solvates, stereoisomers, tautomers, cis-trans isomers, isotope-labeled compounds, and prodrugs for the preparation of pharmaceutical compositions in various administration forms.

Benefits of technology

It improves the metabolic stability and biological activity of the compound, extends the dosing interval, and can more effectively restore the sensitivity of MSSA and MRSA bacteria to β-lactam drugs, thus enhancing the therapeutic effect of antibiotics.

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Abstract

The invention discloses a compound for recovering sensitivity of beta-lactam antibiotics, a composition and application, and belongs to the field of chemical medicines. The invention provides a boric acid compound with a brand new structure as shown in a formula (I) and a pharmaceutically acceptable salt thereof, on one hand, the boric acid compound has better metabolic stability and biological activity, and the administration time interval is expanded; on the other hand, the method can be better used for interfering a beta-lactam antibiotic reaction pathway, so that MSSA and MRSA bacteria have better sensitivity to lactam drugs.
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