Abstract
The activities of T-1982 (sodium 7 beta-[(2R, 3S)-2-(4-ethyl-2, 3-dioxo-1-piperazine-carboxamido)-3-hydroxybutanamido]-7 alpha-methoxy-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylate) against various gram-positive and gram-negative bacteria were compare with those of cefmetazole, cefoxitin, cefazolin, and cefoperazone. T-1982 was active against both gram-positive and gram-negative bacteria, including genera resistant to the other cephalosporins. T-1982 exhibited greater activity than did cefmetazole, cefoxitin, cefazolin, or cefoperazone against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Serratia marcescens and was also highly active against Bacteroides fragilis. T-1982 was as stable to various beta-lactamases as were cefmetazole and cefoxitin. The therapeutic activities of T-1982 in mice experimentally infected with various gram-negative bacteria were superior to those of cefmetazole, cefoxitin, cefazolin, and cefoperazone.
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Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Hirai K., Iyobe S., Inoue M., Mitsuhashi S. Purification and properties of a new beta-lactamase from Pseudomonas cepacia. Antimicrob Agents Chemother. 1980 Mar;17(3):355–358. doi: 10.1128/aac.17.3.355. [DOI] [PMC free article] [PubMed] [Google Scholar]
- LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [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]
- Nakao H., Yanagisawa H., Shimizu B., Kaneko M., Nagano M. A new semisynthetic 7alpha-methoxycephalosporin, CS-1170: 7beta-((cyanomethyl)thio)acetamido)-7alpha-methoxy-3-((1-methyl-1H-tetrazol-5-yl)thio)methyl)-3-cephem-4-carboxylic acid. J Antibiot (Tokyo) 1976 May;29(5):554–558. doi: 10.7164/antibiotics.29.554. [DOI] [PubMed] [Google Scholar]
- Neu H. C. Cefoxitin, a semisynthetic cephamycin antibiotic: antibacterial spectrum and resistance to hydrolysis by gram-negative beta-lactamases. Antimicrob Agents Chemother. 1974 Aug;6(2):170–176. doi: 10.1128/aac.6.2.170. [DOI] [PMC free article] [PubMed] [Google Scholar]
- PERRET C. J. Iodometric assay of penicillinase. Nature. 1954 Nov 27;174(4439):1012–1013. doi: 10.1038/1741012a0. [DOI] [PubMed] [Google Scholar]
- Richmond M. H., Sykes R. B. The beta-lactamases of gram-negative bacteria and their possible physiological role. Adv Microb Physiol. 1973;9:31–88. doi: 10.1016/s0065-2911(08)60376-8. [DOI] [PubMed] [Google Scholar]
- Ueo K., Fukuoka Y., Hayashi T., Yasuda T., Taki H., Tai M., Watanabe Y., Saikawa I., Mitsuhashi S. In vitro and in vivo antibacterial activity of T-1220, a new semisynthetic penicillin. Antimicrob Agents Chemother. 1977 Oct;12(4):455–460. doi: 10.1128/aac.12.4.455. [DOI] [PMC free article] [PubMed] [Google Scholar]