Gruppo Lepetit S.p.a.

Jurgen K Kettenring

Adriano Malabarba

Romeo Ciabatti

Pierfausto Seneci

Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glyccpeptide antibiotics), Y represents a carboxyacid group, a functional derivative of said carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts. The compounds are obtained by reductive cleavage of the peptidic bond between the second and the third aminoacid of the seven aminoacid chain of dalbaheptides (glycopeptide antibiotics). The inventions concerns also the reductive cleavage process which implies using an alkali metal borohydride as the reagent. The compounds show antibacterial activity against staphylococcal and streptococcal strains.

Pentapeptide antibiotics

The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.

Substituted alkylamide derivatives of teicoplanin

C.sup.63 -Amide derivatives of 34-de(acetylglucosaminyl)-34-deoxy-teicoplanin wherein the amide moiety is derived from a di- or poly-amine. The derivatives are prepared by reacting 34-de(acetylglucosaminyl)- 34-deoxy-teicoplanins with an active esters forming reagent such as chloroacetonitrile and then contacting the resulting active esters with the appropriate di- or poly-amine. The amide derivatives which are active against Gram-positive microorganisms, in particular against Group A Streptococci were found to be active also against bacteria which are resistant to glycopeptide antibiotics.

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Varese, Italy

Jurgen K Kettenring