Antifungal compounds, preparation method therefor, and use thereof

By designing small molecule compounds to form π-S bonds and π-π interactions with lanolin alcohol demethylase, and introducing heterocyclic structures at the ends, the problems of low efficacy and solubility of antifungal drugs against drug-resistant fungi were solved, achieving highly efficient inhibition of drug-resistant fungi and reduction of inflammatory responses.

WO2026107624A1PCT designated stage Publication Date: 2026-05-28SHANGHAI JIAOTONG UNIV
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
SHANGHAI JIAOTONG UNIV
Filing Date
2024-11-19
Publication Date
2026-05-28

AI Technical Summary

Technical Problem

Existing antifungal drugs are ineffective against drug-resistant fungi and have problems with low solubility and rapid metabolism. At the same time, deep fungal infections can cause severe inflammatory responses, affecting patients' health.

Method used

A class of small molecule compounds was designed to form π-S bonds with lanolin alcohol demethylase by introducing disulfide bonds, and to introduce heterocyclic structures at the ends to enhance the interaction with the target. At the same time, steric hindrance was introduced at the α-position to improve the metabolic stability of the compounds, and water solubility was improved by salt formation.

Benefits of technology

The compound exhibits excellent activity against drug-resistant fungi, significantly reduces the expression of the inflammatory factor IL-6, and alleviates the inflammatory response. It is significantly superior to existing drugs such as fluconazole, and has a longer half-life and good water solubility.

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Abstract

Disclosed in the present invention are antifungal compounds, a preparation method therefor, and the use thereof. The compounds have the following general formula I, wherein L represents a linking moiety, referring to a small molecule fragment, and Ar represents a heterocyclic ring or a substituted heterocyclic ring. The series of compounds of the present invention can better bind to an enzyme target by means of various interaction forces, thereby exhibiting good activity; and the compounds exhibit excellent activity in both in vitro experiments and animal experiments, the activity of most of the compounds against Candida albicans being better than that of fluconazole. In addition, the series of compounds have anti-inflammatory effects while eliminating fungal infections; and compared with voriconazole, the series of compounds of the present invention can remarkably down-regulate the expression of an inflammatory factor interleukin 6.
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