Novel macrolide derivatives havaing effect of potentiating antifungal activity
    10.
    发明申请
    Novel macrolide derivatives havaing effect of potentiating antifungal activity 失效
    新型大环内酯衍生物具有增强抗真菌活性的作用

    公开(公告)号:US20050176655A1

    公开(公告)日:2005-08-11

    申请号:US10472044

    申请日:2002-10-29

    CPC分类号: C07H17/08 A61K31/7048

    摘要: Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]: wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.

    摘要翻译: 大环内酯衍生物对唑类抗真菌剂的活性具有增强的作用,在低浓度和短时间内对真菌感染起作用,并降低抗性微生物出现的频率。 一种这样的物质是由式[I]表示的化合物:其中R1是Ac,R2和R3是Ac,R4是Me; 当R1为H时,R2和R3为Ac,R4为Me; 当R1为H时,R2和R3为Ac,R4为H时,当R1Bz1,R2和R3为Bz1,R4为Me时; 当R1为Ac时,R2和R3为Pr,R4为Me; 当R1为Ac时,R2和R3为Hex,R4为Me; 当R1为Ac时,R2和R3为Bz1,R4为Me; 当R1为H时,R2和R3为Pr,R4为Me; 当R1为H时,R2和R3为Hex,R4为Me; 当R1为H时,R2和R3为Bz1,R4为Me; 当R1为H时,R2为H,R3为Bz1,R4为Me; 当R1为H时,R2和R3为Hex,R4为H,或当R1为H时,R2和R3为Hex,R4为Et。