CHEMICAL MODIFICATION OF ERYTHROMYCINS: III. IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITIES OF NEW SEMISYNTHETIC 6-O-METHYLERYTHROMYCINS A, TE-031 (CLARITHROMYCIN) AND TE-032

The in vitro and in vivo antibacterial activities of 6-O-methylerythromycin A (TE-031, A-56268, or clarithromycin) and 6, 11-di-O-methylerythromycin A (TE-032) have been compared with those of erythromycin A (EM) and josamycin (JM). TE-031 and TE-032, having the same antibacterial spectra as EM, are...

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Bibliographic Details
Published in:Journal of antibiotics 1990/03/25, Vol.43(3), pp.295-305
Main Authors: MORIMOTO, SHIGEO, NAGATE, TAKATOSHI, SUGITA, KAZUHIKO, ONO, TAKEO, NUMATA, KAZUO, MIYACHI, JUNKO, MISAWA, YOKO, YAMADA, KENJI, OMURA, SADAFUMI
Format: Article
Language:English
Subjects:
Animals
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Bacteria - drug effects
Biological and medical sciences
Clarithromycin
Dogs
Erythromycin - analogs & derivatives
Erythromycin - pharmacokinetics
Erythromycin - pharmacology
Erythromycin - therapeutic use
Hydrogen-Ion Concentration
Josamycin - pharmacokinetics
Josamycin - pharmacology
Josamycin - therapeutic use
Male
Medical sciences
Mice
Mice, Inbred ICR
Pharmacology. Drug treatments
Rabbits
Rats
Rats, Inbred Strains
Staphylococcal Infections - drug therapy
Streptococcal Infections - drug therapy
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Summary:The in vitro and in vivo antibacterial activities of 6-O-methylerythromycin A (TE-031, A-56268, or clarithromycin) and 6, 11-di-O-methylerythromycin A (TE-032) have been compared with those of erythromycin A (EM) and josamycin (JM). TE-031 and TE-032, having the same antibacterial spectra as EM, are active against aerobic Gram-positive bacteria, some Gram-negative bacteria, anaerobic bacteria, L-form bacteria and Mycoplasmapneumoniae. The activity of TE-031 against clinical isolates is equal to or two times more potent than that of EM, whereas TE-032 is slightly less active than EM. The activities of TE-031 and TE-032 are pH dependent (more active at pH 8 than at 5) and are increased by adding serum to medium. TE-031 and TE-032 show dose-related bactericidal activities against Haemophilus influenzae. The therapeutic efficacies of TE-031 and TE-032 against systemic and subcutaneous infections provoked by Gram-positive bacteria in mice are 4- to 35-fold superior to those of EM and JM. TE-031 and TE-032 have demonstrated higher and longer-lasting plasma levels than EM when administered orally to mice, rats or dogs.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.43.295