A preparation method and use of aromatic iminothiazole compounds

By synthesizing arylimidothiazoles compounds and their salts, the problem of insufficient therapeutic effect of existing antibiotics on multidrug-resistant bacteria has been solved, and the efficiency and water solubility of polymyxin E and daptomycin are improved, which is suitable for the treatment of multidrug-resistant Gram-negative and positive bacteria infections.

CN115124487BActive Publication Date: 2025-09-05EAST CHINA UNIV OF SCI & TECH +1
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Patent Information

Application Number
CN202110315644.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2021-03-24
Publication Date
2025-09-05
Estimated Expiration
2041-03-24

AI Technical Summary

Technical Problem

The existing antibiotics have limited therapeutic effects on multidrug-resistant Gram-negative and Gram-positive bacteria and have toxicity problems, and new synergists need to be developed to improve therapeutic effects and reduce toxicity.

Method used

Synthesis of an aromatic iminothiazole compound and its pharmaceutically acceptable salts enhances the antibacterial effect of polymyxin E and daptomycin, and improves its water solubility by forming salts to improve drug properties.

Benefits of technology

The compounds significantly enhance the antibacterial activity against polymyxin E and daptomycin, reduce the risk of toxicity, and increase water solubility, making them suitable for clinical treatment of multidrug-resistant bacteria infection.

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Abstract

The present invention provides an aryliminothiazole compound represented by Formula I or a pharmaceutically acceptable salt thereof, as well as a preparation method and use thereof. These compounds or pharmaceutically acceptable salts thereof can simultaneously enhance the activity of polymyxin E against Gram-negative bacteria and daptomycin against Gram-positive bacteria, and can be used in the antibacterial treatment of pathogens that are insensitive to polymyxins. #imgabs0#
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