Basic monocarboxyamide derivatives of actagardine having antibio

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514222, 514228, 514252, 514255, 514316, 514331, 514422, 514428, 514542, 514550, 514562, 514570, 424117, 544 581, 544 585, 544 586, 544 85, 544111, 544121, 544130, 544141, 544159, 544357, 544359, 544360, 544364, 544372, 544400, 546190, 546208, 546233, 548523, 548567, 548568, 548950, 560 9, 560147, 562426, 562556, A61K 3574, A61K 3500, C07D29514

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046846441

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 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.

REFERENCES:
patent: 4022884 (1977-05-01), Parenti et al.
Malabarba et al., Chemical Abstracts, vol. 104, (1986), No. 48401z.

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