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    Polysubstituted thiazolylpyridine carboxyamide antifungal antibiotic
    7.
    发明授权
    Polysubstituted thiazolylpyridine carboxyamide antifungal antibiotic 失效
    多取代噻唑吡啶羧酰胺抗真菌抗生素

    公开(公告)号：US4956374A

    公开(公告)日：1990-09-11

    申请号：US226016

    申请日：1988-07-29

    申请人： Maki Nishio ,  Shigeyuki Ando ,  Takeo Miyaki ,  Masataka Konishi ,  Toshikazu Oki

    发明人： Maki Nishio ,  Shigeyuki Ando ,  Takeo Miyaki ,  Masataka Konishi ,  Toshikazu Oki

    IPC分类号： C07D417/04 ,  C12P17/16

    CPC分类号： C07D417/04 ,  C12P17/16 ,  C12R1/01

    摘要： Novel antifungal antibiotic compounds have the structural formula ##STR1## A preferred compound where R is 4-hydroxypentyl is denoted BU-3557B.sub.2. A complex of said compounds is produced by fermenting a culture of Sacchrothrix aerocolonigenes strain N806-4 (ATCC 53712). The complex is recovered by adsorption on nonionic porous polymer resin adsorbent and individual component compounds exhibit in vitro activity against fungi and Gram-positive bacteria and BU-3557B.sub.2 demonstrates in vitro antiprotazoal activity. BU-3557B.sub.2 demonstrates in vivo activity against C. albicans vaginal infection and BU-3557A.sub.3 (where R is 1,5-dihydroxy-5,5-dimethylpentyl) demonstrates in vivo activity against C. albicans systemic infection.

    摘要翻译： 新型抗真菌抗生素化合物具有结构式：其中R为4-羟基戊基的优选化合物为BU-3557B2。 通过发酵产气荚膜梭菌菌株N806-4（ATCC 53712）的培养物产生所述化合物的复合物。 通过非离子多孔聚合物树脂吸附剂上的吸附回收复合物，并且各组分化合物表现出对真菌和革兰氏阳性细菌的体外活性，并且BU-3557B2证明体外抗原辅素生物活性。 BU-3557B2证明体内活性针对白色念珠菌阴道感染和BU-3557A3（其中R为1,5-二羟基-5,5-二甲基戊基）表现出对白色念珠菌全身感染的体内活性。