Abstract
The antibacterial activities of K-4619 (3-de-O-methylsporaricin A sulfate) were compared with those of sporaricin A, amikacin, dibekacin, and gentamicin. K-4619 exhibited a high order of activity against gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa. Its activity against Providencia species and Serratia marcescens was the highest of all drugs tested. K-4619 was highly effective against bacteria that produce various aminoglycoside-inactivating enzymes, except for 3-acetyltransferase I. The bactericidal activity of K-4619 was somewhat greater than that of amikacin. The activity of K-4619 against gram-negative bacteria increased at alkaline pH and was hardly affected by inoculum size, addition of horse serum, and composition of the medium. The in vivo protective effect of K-4619 against infections with Klebsiella pneumoniae, S. marcescens, and P. aeruginosa in mice was greater than that of sporaricin A. K-4619 was also active in mice infected with gentamicin- or amikacin-resistant strains bearing some of the aminoglycoside-inactivating enzymes.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Deushi T., Iwasaki A., Kamiya K., Kunieda T., Mizoguchi T., Nakayama M., Itoh H., Mori T., Oda T. A new broad-spectrum aminoglycoside antibiotic complex, sporaricin. I. Fermentation, isolation and characterization. J Antibiot (Tokyo) 1979 Mar;32(3):173–179. doi: 10.7164/antibiotics.32.173. [DOI] [PubMed] [Google Scholar]
- Girolami R. L., Stamm J. M. Comparative antimicrobial activity of O-demethylfortimicin A, a derivative of fortimicin A. Antimicrob Agents Chemother. 1980 Nov;18(5):766–772. doi: 10.1128/aac.18.5.766. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Horiuchi Y., Ikeda D., Kondo S., Umezawa H. Synthesis of the 3-O-demethyl and 2"-N-formimidoyl derivatives of istamycin B. J Antibiot (Tokyo) 1980 Dec;33(12):1577–1580. doi: 10.7164/antibiotics.33.1577. [DOI] [PubMed] [Google Scholar]
- Ikeda D., Horiuchi Y., Kondo S., Umezawa H. Synthesis of demethyl derivatives of istamycin A. J Antibiot (Tokyo) 1980 Nov;33(11):1281–1288. doi: 10.7164/antibiotics.33.1281. [DOI] [PubMed] [Google Scholar]
- Jones R. N., Thornsberry C., Barry A. L., Packer R. R., Baker C. N., Badal R. E. Compound A49759, the 3-O-demethyl derivative of fortimicin A: in vitro comparison with six other aminoglycoside antibiotics. Antimicrob Agents Chemother. 1980 Nov;18(5):773–779. doi: 10.1128/aac.18.5.773. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kobayashi F., Saino Y., Koshi T., Hattori Y. In vitro and in vivo antimicrobial activities of sporaricin A, a new aminoglycoside. Antimicrob Agents Chemother. 1980 Mar;17(3):337–343. doi: 10.1128/aac.17.3.337. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kobayashi F., Yamaguchi M., Mitsuhashi S. Phosphorylated inactivation of aminoglycosidic antibiotics by Pseudomonas aeruginosa. Jpn J Microbiol. 1971 May;15(3):265–272. doi: 10.1111/j.1348-0421.1971.tb00578.x. [DOI] [PubMed] [Google Scholar]
- Martin J. R., Johnson P., Tadanier J., Goldstein A. Synthesis of 3-O-demethylfortimicins. Antimicrob Agents Chemother. 1980 Nov;18(5):761–765. doi: 10.1128/aac.18.5.761. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ohashi Y., Kawabe H., Sato K., Nakamura N., Kurashige S., Mitsuhashi S. In vitro and in vivo antibacterial activity of KW1070, a new aminoglycoside antibiotic. Antimicrob Agents Chemother. 1980 Feb;17(2):138–143. doi: 10.1128/aac.17.2.138. [DOI] [PMC free article] [PubMed] [Google Scholar]