1984/01/01 by SHIGEO MORIMOTO, Shigeo Morimoto, YOKO TAKAHASHI +4 · 5 citations
Biochemistry, Genetics and Molecular Biology · Chemistry · Medicine · #Cancer therapeutics and mechanisms #Pneumonia and Respiratory Infections #Synthesis and Biological Evaluation
paper · pdf · doi:10.7164/antibiotics.37.187
crossref issued 1984/01/01 · crossref published 1984/01/01 · crossref published-print 1984/01/01 · openalex publication_date 1984/01/01 · crossref created 2012/02/29 · crossref deposited 2012/02/29 · openalex created_date 2025/10/10 · crossref indexed 2026/07/31 · openalex updated_date 2026/08/01
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.