Indole-based chalcone compounds as antibacterial agents

    公开(公告)号:US11731939B1

    公开(公告)日:2023-08-22

    申请号:US18118280

    申请日:2023-03-07

    摘要: The indole-based chalcone compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

    ANTIFUNGAL PRODRUGS
    56.
    发明公开
    ANTIFUNGAL PRODRUGS 审中-公开

    公开(公告)号:US20230218652A1

    公开(公告)日:2023-07-13

    申请号:US17927941

    申请日:2021-05-28

    IPC分类号: A61K31/7048 A61P31/10

    CPC分类号: A61K31/7048 A61P31/10

    摘要: The invention relates to an antifungal prodrug which comprises an antifungal moiety which is linked to a trigger moiety by means of a self-immolative spacer. The trigger moiety is selected from glycosyl residues and oligosaccharides, stabilizes the self-immolative spacer and is cleavable by a pathogen hydrolytic enzyme which is preferably an extracellular glycosidase (EC 3.2.1). When the trigger moiety is cleaved by the pathogen hydrolytic enzyme, the self-immolative spacer undergoes a spontaneous degradation so as to release the antifungal moiety. The invention also relates to pharmaceutical compositions comprising said prodrug and to its use in the treatment of infectious diseases.