Synthesis and Structure-activity Relationships of 1.BETA.-Methylcarbapenems with Quaternary Ammonium Side Chains.
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- ISHIKAWA KATSUYA
- Research Laboratories, Sankyo Co., Ltd.
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- KOJIMA KATSUHIKO
- Research Laboratories, Sankyo Co., Ltd.
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- MIYAUCHI MASAO
- Research Laboratories, Sankyo Co., Ltd.
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- ENDO ROKURO
- Research Laboratories, Sankyo Co., Ltd.
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- YASUDA HIROSHI
- Research Laboratories, Sankyo Co., Ltd.
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- KAWAMOTO ISAO
- Research Laboratories, Sankyo Co., Ltd.
抄録
The synthesis and antibacterial activity of 1β-methylcarbapenems with quaternary ammonium groups at the C-2 position have been studied. Two types of new carbapenem derivatives have been synthesized. These 1β-methylcarbapenems, one type having a (2S, 4S)-2-[1, 1-dimethyl-2-(1-piperazinyl)carbonyl]pyrrolidinio-4-ylthio group and the other type having a (2S, 4S)-2-(4-carbamoylmethyl-4-methylhomopiperazinio-1-ylcarbonyl)pyrrolidin-4-ylthio group, show potent and well balanced antibacterial activity as well as high stability against dehydropeptidase-I. The in vivo potency of these two carbapenems was compared with that of meropenem. The structure-activity relationships leading to these carbapenems are also described.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 51 (8), 757-770, 1998
公益財団法人 日本感染症医薬品協会