Antifungal prodrugs

The present invention relates to an antifungal prodrug comprising an antifungal moiety linked to a trigger moiety using a self-dissociating spacer. And a trigger moiety selected from glycosyl residues and oligosaccharides, stabilising the self-dissociating spacer and capable of being cleaved by a pa...

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Bibliographic Details
Main Authors GRATIEN GILLES-OLIVIER, LE PAPE PATRICE, TEISSIER, ARNAUD, LEBRETON JACQUES, PANIER FABRICE
Format Patent
LanguageChinese
English
Published 17.03.2023
Subjects
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The present invention relates to an antifungal prodrug comprising an antifungal moiety linked to a trigger moiety using a self-dissociating spacer. And a trigger moiety selected from glycosyl residues and oligosaccharides, stabilising the self-dissociating spacer and capable of being cleaved by a pathogen hydrolase, preferably an extracellular glycosidase (EC 3.2. 1). When the trigger moiety is cleaved by the pathogen hydrolase, the self-decomposing spacer undergoes spontaneous degradation in order to release the antifungal moiety. The invention also relates to a pharmaceutical composition containing the prodrug and application of the prodrug in treating infectious diseases. 本发明涉及一种抗真菌前体药物，其包含利用自分解间隔物与触发组成部分相连的抗真菌组成部分。所述触发组成部分选自糖基残基和寡糖，使所述自分解间隔物稳定，并且能够被病原体水解酶、优选为细胞外糖苷酶(EC 3.2.1)切割。当所述触发组成部分被所述病原体水解酶切割时，所述自分解间隔物经历自发降解，以便释放出所述抗真菌组成部分。本发明还涉及包含所述前体药物的药物组合物及其在治疗传染病中的用途。
Bibliography:Application Number: CN202180037813