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
| Autor: | Kazuo Numata, Yoko Misawa, Kazuhiko Sugita, Sadafumi Omura, Junko Miyachi, Kenji Yamada, Takeo Ono, Takatoshi Nagate, Shigeo Morimoto |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Josamycin Stereochemistry medicine.drug_class Antibiotics Erythromycin Biology Microbiology Mice Dogs In vivo Clarithromycin Streptococcal Infections Drug Discovery medicine Animals Pharmacology Mice Inbred ICR Bacteria Biological activity Rats Inbred Strains Hydrogen-Ion Concentration Staphylococcal Infections biology.organism_classification Rats Anaerobic bacteria Rabbits medicine.drug |
| Zdroj: | The Journal of antibiotics. 43(3) |
| ISSN: | 0021-8820 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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