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.