Novel dithiocarbamate carbapenems with anti-MRSA activity

Autor: Ohtake, Norikazu, Imamura, Hideaki, Jona, Hideki, Kiyonaga, Hideo, Shimizu, Aya, Moriya, Minoru, Sato, Hiroki, Nakano, Masato, Ushijima, Ryosuke, Nakagawa, Susumu
Zdroj: Bioorganic & Medicinal Chemistry; July 1998, Vol. 6 Issue: 7 p1089-1101, 13p
Abstrakt: A new series of 1β-methyl carbapenems, in which a disubstituted-aminothiocarbonylthio moiety was attached to the C-2 position of the carbapenem nucleus, were prepared and evaluated for anti-MRSA activity. These derivatives showed good in vitro antibacterial activity against high-level MRSA, and the finding of good affinity for PBP-2′ supported these results. Some of the compounds having favorable protein-binding affinity showed excellent in vivo anti-MRSA activity.
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