Rapamycin derivative as well as preparation method and application thereof

The invention relates to the field of medicine synthesis, in particular to a rapamycin derivative as well as a preparation method and application thereof. The rapamycin derivative is 40-O-(3-(4-piperidinecarboxylate)-1H-1, 2, 3-triazole-1-yl)) ethyl rapamycin, the structural formula of the rapamycin...

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Bibliographische Detailangaben
Hauptverfasser: CHEN XIAOMING, YANG GUOXIN, HUANG JIE, YING JIAYIN, CHEN XIAQIN, JIN DONGWEI, CHEN YOUZHONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the field of medicine synthesis, in particular to a rapamycin derivative as well as a preparation method and application thereof. The rapamycin derivative is 40-O-(3-(4-piperidinecarboxylate)-1H-1, 2, 3-triazole-1-yl)) ethyl rapamycin, the structural formula of the rapamycin derivative is shown in the specification, and the in-vitro antibacterial biological activity of the rapamycin derivative shows that the rapamycin derivative has antibacterial activity. Compared with rapamycin, the compound not only has the activity of inhibiting fungi, but also has better activity of inhibiting bacteria. 本发明涉及药物合成领域,尤其涉及一种雷帕霉素衍生物及其制备方法和应用。所述雷帕霉素衍生物为40-O-(3-(4-哌啶甲酸乙酯基)-1H-1,2,3-三氮唑-1-基))乙基雷帕霉素,其结构式如下:本发明的雷帕霉素衍生物,体外抑菌生物学活性显示其具有抗菌活性。与雷帕霉素相比,不仅具有抑制真菌的活性,还具有较好的抑制细菌的活性。