Synthesis of novel di- and tricationic carbapenems with potent anti-MRSA activity |
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Authors: | Takahisa Maruyama Yasuo Yamamoto Yuko Kano Mizuyo Kurazono Eiki Shitara Katsuyoshi Iwamatsu Kunio Atsumi |
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Institution: | 1. Process Development Section Kitakami-Plant, Meiji Seika Kaisha, Ltd., 3-3 Kita-Kougyoudanchi, Kitakami-shi, Iwate 024-0012, Japan;2. Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan |
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Abstract: | A new series of 1β-methyl carbapenems possessing a 6,7-disubstituted imidazo5,1-b]thiazol-2-yl group directly attached to the C-2 position of the carbapenem nucleus was prepared, and their activities against methicillin-resistant Staphylococcus aureus (MRSA) were evaluated. First, a benzyl moiety was introduced at the C-6 position of imidazo5,1-b]thiazole attached to the carbapenem. These benzylated molecules showed potent anti-MRSA activity, but poor water solubility. In order to overcome this drawback, we designed and synthesized di- and tricationic carbapenems and finally discovered a novel carbapenem (15i), which exhibited excellent anti-MRSA activity and good water solubility. |
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