AMINOGLYCOSIDES

摘要

1530643 Aminoglycosides UPJOHN CO 19 Aug 1976 [8 Sept 1975] 34527/76 Heading C2C Novel aminoglycosides of the general formula wherein T is hydrogen or an amino blocking group; Q is T as defined above or a group of the formula in which n is one, 2 or 3; either W and X are both H or optionally substituted hydrocarboncarboxylic acid acyl radicals of from 2 to 18 carbon atoms and any substituent is selected from halogen, nitro, hydroxy, amino, cyano, thiocyanato and alkoxy or W is hydrogen and X is a glycosyl group selected from pentafuran. osyl, hexapyranosyl and aminopyranosyl of the formula wherein R 1 is hydroxy, acetyloxy, benzoyloxy, benzyloxy, amino, acylamino of from one to 8 carbon atoms, alkylamino of from one to 5 carbon atoms or N-alkylacylamino in which the acyl group is of one to 8 carbon atoms and the alkyl group is of one to 5 carbon atoms and R 2 is hydrogen or acetyl, with the provisos that R 1 is not amino at the 311 or 311 and 611 positions when R 1 at the other positions is hydroxy and that Y is not D-glycosyl; either Y is hydrogen or glycosyl as defined above and Z is hydrogen or Y and Z are taken together and are -CL 1 L 2 - (L 1 and L 2 are alkyl and the total number of C atoms in CL 1 L 2 is not more than 8) with the overall provisos (1) that when W and X are both optionally substituted hydrocarbon-carboxylic acid acyl radicals and Q is then Y is glycosyl and Z is hydrogen; (2) that X and Y are not both glycosyl; (3) that T is not hydrogen when Y and Z are -CL 1 L 2 - or W, and X are both optionally substituted hydrocarbon-carboxylic acyl radicals and Y and Z are both hydrogen; and (4) that when T is H then W and X are both H and non- toxic pharmaceutically acceptable acid addition salts thereof are prepared by removing protecting groups and, if present, acyl groups from a corresponding N-protected and optionally O-acylated compound. They have antibacterial activity and can be included in pharmaceutical compositions.