Synthesis and .BETA.-lactamase inhibitory activity of 6-((1-heteroarylthioethyl-1,2,3-triazol4-yl)methylene)-penam sulfones.
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- IM CHAEUK
- Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta
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- MAITI SAMARENDRA N.
- SynPhar Laboratories Inc.
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- MICETICH RONALD G.
- Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta SynPhar Laboratories Inc.
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- DANESHXALAB MOHSEN
- Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta SynPhar Laboratories Inc.
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- ATCHISON KEVIN
- SynPhar Laboratories Inc.
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- PHILLIPS OLUDOTUN A.
- SynPhar Laboratories Inc.
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- KUNUGITA CHIEKO
- Tokushima Research Center, Taiho Pharmaceutical Company Ltd.
抄録
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.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 47 (9), 1030-1040, 1994
公益財団法人 日本感染症医薬品協会