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

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

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.