title: Synthesis and structure-activity studies of new 4''-O-acyltylosin derivatives of therapeutic interest.
abstract: Eleven 4''-O-acyltylosin derivatives were synthesized and subjected to a two-step screening system consisting of antimicrobial activity and esterase stability assays. The new derivatives were all active against macrolide-resistant Staphylococci and mycoplasmas, but only 4''-O-(4-methoxy)phenylacetyltylosin and 4''-O-(4-acetyl)phenylacetyltylosin showed better resistance to mouse liver esterase than 4''-O-phenylacetyltylosin (reference compound C).
authors.affiliation: Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Yoshioka
authors.forename: K
authors.initials: K
authors.lastname: Kiyoshima
authors.forename: M
authors.initials: M
authors.lastname: Maeda
authors.forename: M
authors.initials: M
authors.lastname: Sakamoto
authors.forename: T
authors.initials: T
authors.lastname: Ishikura
authors.forename: Y
authors.initials: Y
authors.lastname: Fukagawa
authors.forename: T
authors.initials: T
authors.lastname: Sawa
authors.forename: M
authors.initials: M
authors.lastname: Hamada
authors.forename: H
authors.initials: H
authors.lastname: Naganawa
authors.forename: T
authors.initials: T
authors.lastname: Takeuchi
mesh_terms: D000818:Animals; D001419:Bacteria / Q000187:drug effects; D004950:Esterases / Q000494:pharmacology; D007933:Leucomycins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: D007933:Leucomycins; D004950:Esterases