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    • 32. 发明授权
    • Basic monocarboxyamide derivatives of actagardine having antibiotic
activity and compositions thereof
    • 具有抗生素活性的卡那定的基本单羧酰胺衍生物及其组合物
    • US4684644A
    • 1987-08-04
    • US842523
    • 1986-03-21
    • Adriano MalabarbaBruno Cavalleri
    • Adriano MalabarbaBruno Cavalleri
    • C07G11/00A61K35/74A61P31/04C12P1/06A61K35/00C07D295/14
    • C12P1/06
    • The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine. More particularly, they are basic monoamide derivatives of actagardine which may be schematically represented by the following formula I: ##STR2## The compound of the invention possess improved antimicrobial activity in particular against gram positive bacteria.
    • 本发明涉及一类基本的单加酰胺酰胺衍生物。 放线菌肽(INN)是一种抗生素,由Actinoplanes Sp。 ATCC 31048和Actinoplanes Sp。 ATCC 31049,其描述于美国专利No. 第4,022,884号。 阿卡加丁显示抗革兰氏阳性生物的体外和体内活性。 其完整的化学结构尚不清楚,但只有其化学功能和主要碎片的信息。 特别地,已经发现,阿格达加胺具有两个羧基官能团和伯氨基官能团,因此可以表示如下:本发明的化合物是在加马丁的羧​​基官能团之一的单酰胺衍生物。 更具体地说,它们是阿加豆苷的碱性单酰胺衍生物,其可以由下式I示意性地表示:式I本发明的化合物具有改善的抗菌活性,特别是抗革兰氏阳性细菌。