Condensn products of erythromycyl-amine with aldehydes - antibiotic erythromycin derivs active against gram negative and gram positive bacteria

摘要

Erythromycin derivs. of formulae (I) (Ia) and (Ib) and their acid addition salts are novel. R=hydroxy, phenoxy, phenyl 1-3C alkoxy, 1-4C alkoxy a gp. hydroxyalkoxy, alkoxyalkoxy, dialkylaminoalkoxy or alkoxycarbonylalkoxy having 1-4C atoms in the alkylene part and 1-3C atoms in the alkyl part, mercapto, phenylmercapto (opt. substd. by methyl, methoxy, ethoxy, isopropoxy ro propoxy), phenyl-1-3 alkylmercapto, 1-5C straight or branched, alkylmercapto, cyclohexylmercapto, a gp. hydroxyalkylmercapto, dialkylaminomercapto, alkoxycarbonylalkylmercapto or cyanoalkylmercapto in each case having 1-3C in the alkyl or alkylene parts, -NR2R3, R4-COO, -NH-CO-R5, N-phenylcarbamoyl, R6R7-N-CO-CH2-O-, (R8O)2=P(O)-, -NH-SO2-R9 or -SO2-R10; R2, R3=H, phenyl phenyl-1-3C alkyl, 1-4C alkyl or NR2R3 form a 5-6 membered monocyclic heterocyclic opt. contg. a O or S or another N; R4=(un)branched 1-5C alkyl, benzyl or phenyl; R5=(un)branched 1-5c alkyl opt. substd. by 1 or 2 halo atoms or by a cyano gp., phenyl-1-3C-alkyl opt. substd. in the phenyl ring by 1-2 halo atoms or by a methoxy gp. and in the alkylene part by a halo atom, phenoxy-1-3C alkyl, phenyl-2-4C alkenyl, phenyl(opt. substd. by methyl, hydroxy, methoxy, nitro or chloro gps.), pyridyl, furyl, fluorofuryl or thienyl; R6,R7=methyl, ethyl, propyl or isopropyl; R8=(un)branched 1-5c alkyl, R9=1-4C alkyl or phenyl opt. substd. by a 1-3c alkyl; and R10=1-3C alkyl or phenyl opt. substd. by a 1-3C alkyl gps. Cpds. are antibacterials having good activity against Gram. positive and Gram-negative organisms.