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    • 10. 发明申请
    • Novel macrolide derivatives havaing effect of potentiating antifungal activity
    • 新型大环内酯衍生物具有增强抗真菌活性的作用
    • US20050176655A1
    • 2005-08-11
    • US10472044
    • 2002-10-29
    • Satoshi OmuraHiroshi TomodaToshiaki SunazukaMasayoshi AraiTohru Nagamitsu
    • Satoshi OmuraHiroshi TomodaToshiaki SunazukaMasayoshi AraiTohru Nagamitsu
    • A01N43/04A61K31/7048A61P31/10C07H17/08
    • C07H17/08A61K31/7048
    • 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.
    • 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。