Abstract
BO-1236, a new cephalosporin having an N-methyl-5,6-dihydroxyisoindolinium moiety on the 3-methylene of the cephem, showed potent activity against gram-negative organisms, including Pseudomonas aeruginosa. The in vitro activity of BO-1236 was superior or comparable to that of ceftazidime, cefotaxime, and cefoperazone in susceptibility tests with clinical isolates. BO-1236 was significantly more active than ceftazidime against P. aeruginosa strains susceptible or resistant to ceftazidime or gentamicin or both. MBCs were usually close to MICs, both of which were influenced by inoculum size to about the same degree as those of the other beta-lactams. BO-1236 was stable to all types of beta-lactamases except type I oxyiminocephalosporin-hydrolyzing enzyme, by which BO-1236 was slightly hydrolyzed. BO-1236 showed protective activity superior to that of ceftazidime and cefotaxime in experimental infections in mice caused by two strains of P. aeruginosa and showed activity comparable to that of ceftazidime and cefotaxime against other gram-negative bacterial infections.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Chopra I., Howe T. G., Linton A. H., Linton K. B., Richmond M. H., Speller D. C. The tetracyclines: prospects at the beginning of the 1980s. J Antimicrob Chemother. 1981 Jul;8(1):5–21. doi: 10.1093/jac/8.1.5. [DOI] [PubMed] [Google Scholar]
- Matsubara N., Minami S., Muraoka T., Saikawa I., Mitsuhashi S. In vitro antibacterial activity of cefoperazone (T-1551), a new semisynthetic cephalosporin. Antimicrob Agents Chemother. 1979 Dec;16(6):731–735. doi: 10.1128/aac.16.6.731. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mitsuhashi S., Inoue M., Masuyoshi S. Antibacterial activity of cefotaxime. J Antimicrob Chemother. 1980 Sep;6 (Suppl A):37–46. doi: 10.1093/jac/6.suppl_a.37. [DOI] [PubMed] [Google Scholar]
- Neu H. C., Aswapokee N., Aswapokee P., Fu K. P. HR 756, a new cephalosporin active against gram-positive and gram-negative aerobic and anaerobic bacteria. Antimicrob Agents Chemother. 1979 Feb;15(2):273–281. doi: 10.1128/aac.15.2.273. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Neu H. C., Fu K. P., Aswapokee N., Aswapokee P., Kung K. Comparative activity and beta-lactamase stability of cefoperazone, a piperazine cephalosporin. Antimicrob Agents Chemother. 1979 Aug;16(2):150–157. doi: 10.1128/aac.16.2.150. [DOI] [PMC free article] [PubMed] [Google Scholar]
- O'Callaghan C. H. Description and classification of the newer cephalosporins and their relationships with the established compounds. J Antimicrob Chemother. 1979 Nov;5(6):635–671. doi: 10.1093/jac/5.6.635. [DOI] [PubMed] [Google Scholar]
- Preheim L. C., Penn R. G., Sanders C. C., Goering R. V., Giger D. K. Emergence of resistance to beta-lactam and aminoglycoside antibiotics during moxalactam therapy of Pseudomonas aeruginosa infections. Antimicrob Agents Chemother. 1982 Dec;22(6):1037–1041. doi: 10.1128/aac.22.6.1037. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Saino Y., Inoue M., Mitsuhashi S. Purification and properties of an inducible cephalosporinase from Pseudomonas maltophilia GN12873. Antimicrob Agents Chemother. 1984 Mar;25(3):362–365. doi: 10.1128/aac.25.3.362. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wise R., Andrews J. M., Bedford K. A. Comparison of in vitro activity of GR 20263, a novel cephalosporin derivative, with activities of other beta-lactam compounds. Antimicrob Agents Chemother. 1980 May;17(5):884–889. doi: 10.1128/aac.17.5.884. [DOI] [PMC free article] [PubMed] [Google Scholar]