Basic monocarboxyamide derivatives of actagardine having...

Details Basic monocarboxyamide derivatives of actagardine having... Basic monocarboxyamide derivatives of actagardine having...

C - Chemistry, Metallurgy

07

G

260/1.39

C07G 11/00 (2006.01) C12P 1/06 (2006.01)

Patent

CA 1259985

ABSTRACT 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 US patent 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: Image 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: Image Formula I The compounds of the invention possess improved antimicrobial activity in particular against gram positive bacteria.

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