In vitro activity of YM133, a new semisynthesized macrolide.
YM133, the 4"-O-(4-methoxyphenyl)acetyltylosin, is a new macrolide. The in vitro activity of YM133 was compared with those of erythromycin, josamycin, and rokitamycin by an agar dilution method. YM133 inhibited 90% of the tested isolates of Streptococcus pneumoniae, Legionella spp., and anaerobic bacteria at less than or equal to 1.56 micrograms/ml. The drug inhibited 90% of erythromycin-resistant staphylococci and Streptococcus pyogenes at less than or equal to 50 micrograms/ml. YM133 showed activity against erythromycin-, josamycin-, and rokitamycin-resistant (MIC greater than or equal to 100 micrograms/ml) strains of staphylococci, streptococci, Bacteroides spp., and Clostridium spp. Enterococci were less susceptible to other YM133-like macrolides. Unlike other macrolides, YM133 showed killing activity, and the MBC/MIC ratios of YM133 for several strains were 1:32, whereas those of erythromycin were 4:1,024. In a time-kill curve study, the reduction of viable cells started within 2 h after the addition of YM133.
Terasawa
T
T
Episome Institute, Seta-gun, Japan.
Watanabe
M
M
Okubo
T
T
Mitsuhashi
S
S
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000382:microbiology; D002981:Clindamycin / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D004917:Erythromycin / Q000494:pharmacology; D015570:Josamycin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015644:Miocamycin / Q000031:analogs & derivatives / Q000494:pharmacology; D009827:Oleandomycin / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D015644:Miocamycin; D002981:Clindamycin; D004917:Erythromycin; D015570:Josamycin; D009827:Oleandomycin; C033383:rokitamycin