9-Alkylamino-erythromycin antibiotics - active against gram-positive and gram-negative bacteria

摘要

9-Alkylamino-erythromycins (I) and thier acid addition salts are novel cpds. R3-(CH2)n-CH-CH-NH-E (where E is erythromycyl R1=H opt. branched 1-3C alkyl, 1-5c alkoxy-1-3C alkyl, phenyl or benzyl R2=H, hydroxy, opt. branched 1-3C alkyl or phenyl. R3=1-5C aliphatic acyloxy, benzyloxy opt. branched 1-5c alkoxy, amino, 1-5C monoalkylamino, 2-8C dialkylamino, opt. branched 1-4c hydroxyalkylamino, opt. branched 2-8C di-(hydroxyalkyl)amino, phenyl-1-2C alkylamino, phenylamino (opt. substd. in the phenyl ring by one or more halo, 1-3C alkyl, 1-3C akoxy or hydroxy), 1-5c aliphatic acylamino (opt. substd. by phenyl), benzylamino (the phenyl ring may be substd. by methoxy, halo or carboxy) p-tolylsulphonamino, N',N'-di(1-3c alkyl)-hydrazino where the alkyl radicals together with the N atom may from a 5-6 membered monocyclic heterocyclic gp. opt. containing an O, S or another N atom and opt. substd. on this second N atom, n= 0 or 1 with the condition that when n=0, Ro may also be hydroxy. (I) are antibacterials active against Gram-positive and Gram-negative organisms.