Abstract |
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 Mycoplasma pneumoniae. 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.
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Authors | S Morimoto, T Nagate, K Sugita, T Ono, K Numata, J Miyachi, Y Misawa, K Yamada, S Omura |
Journal | The Journal of antibiotics
(J Antibiot (Tokyo))
Vol. 43
Issue 3
Pg. 295-305
(Mar 1990)
ISSN: 0021-8820 [Print] England |
PMID | 2139023
(Publication Type: Comparative Study, Journal Article)
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Chemical References |
- 6,11-di-O-methylerythromycin A
- Erythromycin
- Clarithromycin
- Josamycin
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Topics |
- Animals
- Bacteria
(drug effects)
- Clarithromycin
- Dogs
- Erythromycin
(analogs & derivatives, pharmacokinetics, pharmacology, therapeutic use)
- Hydrogen-Ion Concentration
- Josamycin
(pharmacokinetics, pharmacology, therapeutic use)
- Male
- Mice
- Mice, Inbred ICR
- Rabbits
- Rats
- Rats, Inbred Strains
- Staphylococcal Infections
(drug therapy)
- Streptococcal Infections
(drug therapy)
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