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Paper | Special issue | Vol 42, No. 2, 1996, pp.645-651
Published online, 1st January, 1970
DOI: 10.3987/COM-95-S61
Synthesis and Biological Evaluation of Sodium 2β-[(2,5-Dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)sulfonylmethyl]-2α-methylpenam-3α-carboxylate 1,1-Dioxide

Eduardo L. Setti, Oludotun A. Phillips, Andhe V. N. Reddy, Chieko Kunugita, Akio Hyodo, Ronald G. Micetich, and Samarendra N. Maiti

*SynPhar Laboratories Inc., 4290-91A Street, Edmonton, Alberta, T6E 5V2, Canada

Abstract

A new β-lactamase inhibitor, sodium 2β-[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)sulfonymethyl]-2α-methylpenam-3α-carboxylate 1,1-dioxide (3). was synthesized. The compound (3) had excellent invitro inhibitory activity except against cephalosporinase. In combination with ampicillin, piperacillin and ceftazidime, its synergistic effects was inferior to tazobactam, thus suggesting poor penetration through the bacterial cell wall.