- 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.