Studies on anti-Helicobacter pylori agents. Part 2: new cephem derivatives |
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Authors: | Yoshida Y Matsuda K Sasaki H Matsumoto Y Matsumoto S Tawara S Takasugi H |
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Affiliation: | Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan. yoshiki_yoshida@po.fujisawa.co.jp |
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Abstract: | The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of cephem derivatives are described. Introduction of thio-heterocyclic groups containing N- and S-atoms to the 3-position and phenyl or thienyl acetamido groups to the 7-position of the cephem nucleus dramatically improved the activity. From this series of derivatives, compound 13i was found to have extremely potent in vitro anti-H. pylori activity, superior therapeutic efficacy compared to AMPC and CAM, no cross-resistance between CAM or MNZ and low potential for causing diarrhea due to instability to beta-lactamase. |
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