著者

CHIEKO KUNUGITA FUSAHIRO HIGASHITANI AKIO HYODO NORIO UNEMI MATSUHISA INOUE

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.48, no.12, pp.1453-1459, 1995-12-25 (Released:2006-04-19)

参考文献数

27

被引用文献数

2 5

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A new extended spectrum β-lactamase was detected in Serratia marcescens 42039 that was isolated from urine of patients with complicated urinary tract infection in Japan. This strain produced three different β-lactamase types (TEM-1, a cephalosporinase, and a new β-lactamase: CKH-1). The TEM-1 and CKH-1 encoding genes were conjugated from S. marcescens 42039 to Escherichia coli K-12 at frequencies of 10-5 to 10-6. The MICs of β-lactams against the transconjugant were: ampicillin >1600, piperacillin 800, cephalothin 1600, ceftazidime 6.25, cefotaxime 100, and ceftriaxone 200μg/ml. The CKH-1 enzyme was purified to more than 90% by ion-exchange chromatography. The molecular weight of purified CKH-1 was 30 K dalton and the isoelectric point was 8, 2, Relative Vmax/Km values (cephaloridme=100) of penicillin G, cephalothin, and oxyiminocephalosporins such as cefuroxime, ceftriaxone, and cefotaxime, were 256, 226, 116, 87, and 49, respectively. The I50 values of tazobactam, BRL-42715, and clavulanic acid against CKH-1 enzyme were 0.0011, 0.0002, and 0.097μM, respectively. The enzymatic activity of CKH-1 was not inhibited by EDTA and anti-TEM-1 serum. These findings indicate that CKH-1 is a member of the groups of class A β-lactamases. This is the first report of a plasmid-mediated oxyiminocephalosporin hydrolyzing broad-spectrum β-lactamase from clinical isolates of S. marcescens.

著者

EDUARDO L. SETTI NARENDER A. V. REDDY OLUDOTUN A. PHILLIPS DAVID P. CZAJKOWSKI KEVIN ATCHISON HARNINDER ATWAL RONALD G. MICETICH SAMARENDRA N. MAITI CHIEKO KUNUGITA AKIO HYODO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.49, no.9, pp.944-946, 1996-09-25 (Released:2006-11-21)

参考文献数

6

被引用文献数

4 5

著者

EDUARDO L. SETTI CHARLES FIAKPUI OLUDOTUN A. PHILLIPS DAVID P. CZAJKOWSKI KEVIN ATCHISON RONALD G. MICETICH SAMARENDRA N. MAITI CHIEKO KUNUGITA AKIO HYODO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.48, no.11, pp.1320-1329, 1995-11-25 (Released:2006-04-19)

参考文献数

19

被引用文献数

3 6

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A series of 2β-[(4-substituted)-l, 2, 3-triazol-l-yl]methyl penicillanic acid sulfones was synthesized as β-lactamase inhibitors. Many of these compounds showed good in vitro inhibitory activity against penicillinase, cefotaximase and plasmid-mediated class III TEM enzymes, but exhibited weaker cephalosporinase inhibition. One member in this series-2β-[(4-pyridiniummethyl)-l, 2, 3-triazol-lyl]methyl-6, 6-dihydropenicillanate 1, 1-dioxide (12a), when tested in combination with piperacillin, showed excellent synergistic activity against microorganisms producing plasmid-mediated enzymes, but had insufficient activity against microorganisms producing chromosomally mediated class I enzymes.

著者

CHAEUK IM SAMARENDRA N. MAITI RONALD G. MICETICH MOHSEN DANESHXALAB KEVIN ATCHISON OLUDOTUN A. PHILLIPS CHIEKO KUNUGITA

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.47, no.9, pp.1030-1040, 1994-09-25 (Released:2006-04-19)

参考文献数

15

被引用文献数

31 42

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The synthesis of β-lactamase inhibitory activity of a series of sodium 6-[(1-heteroarylthioethyl-1, 2, 3-triazol-4-yl)methylene]pemcillanate 1, 1-dioxides are described. Their activity was compared with tazobactam and sulbactam. The Z-isomers were more active than the E-isomers. The in vitro activity of the Z-isomers of the phenylthiadiazole derivatives (13a and 15a) was better than sulbactam against the tested β-lactamases and comparable to tazobactam especially against TEM-2 and cephalosporinase. But their synergistic activity with five antibiotics was inferior to tazobactam.