Synthesis and structure-activity studies of new 4''-O-acyltylosin derivatives of therapeutic interest.
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).
Yoshioka
T
T
Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
Kiyoshima
K
K
Maeda
M
M
Sakamoto
M
M
Ishikura
T
T
Fukagawa
Y
Y
Sawa
T
T
Hamada
M
M
Naganawa
H
H
Takeuchi
T
T
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
D007933:Leucomycins; D004950:Esterases