Erythromycin derivatives

Details Erythromycin derivatives Erythromycin derivatives

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2367319

Erythromycin derivatives of general formula (1) or salts of the same, extremely useful as antimicrobial agents: wherein R is H or lower alkyl; R1 is alkyl, cycloalkyl, (cycloalkyl)alkyl, aralkyl, or -(CH2)n-X-R4; R2 is H or acetyl; R3 is acyl or -C(=O)-Y-R5; R4 is alkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, aryl, or aralkyl; R5 is alkyl, aryl, or aralkyl; n is an integer of 1 to 6; X is O, S, or -NZ-; Y is O or -NH-; and Z is H or alkyl.

L'invention se rapporte à des dérivés d'érythromycine représentés par la formule générale (1), ainsi qu'à des sels de ces dérivés, qui s'avèrent extrêmement utiles en tant qu'agents antimicrobiens. Dans cette formule, R est H ou alkyle inférieur; R?1¿ est alkyle, cycloalkyle, (cycloalkyl)alkyle, aralkyle ou -(CH¿2?)¿n?-X-R?4¿; R?2¿ est H ou acétyle; R?3¿ est acyle ou -C(=O)-Y-R?5¿; R?4¿ est alkyle, alcoxyalkyle, alkylthioalkyle, alkylaminoalkyle, aryle ou aralkyle; R?5¿ est alkyle, aryle ou aralkyle; n est un entier compris entre 1 et 6; X est O, S ou -NZ-; Y est O ou -NH-; et Z est H ou alkyle.

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