ANTIFUNGAL PRODRUGS

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 pathog...

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Bibliographic Details
Main Authors PAGNIEZ, FABRICE, LE PAPE, PATRICE, TESSIER, ARNAUD, LEBRETON, JACQUES, GRATIEN, GILLES-OLIVIER
Format Patent
LanguageEnglish
Published 13.07.2023
Subjects
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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.
Bibliography:Application Number: US202117927941