Author/Authors :
Norikazu Ohtake، نويسنده , , Hideaki Imamura، نويسنده , , Hideki Jona، نويسنده , , Hideo Kiyonaga، نويسنده , , Aya Shimizu، نويسنده , , Minoru Moriya، نويسنده , , Hiroki Sato، نويسنده , , Masato Nakano، نويسنده , , Ryosuke Ushijima، نويسنده , , Susumu Nakagawa، نويسنده ,
Abstract :
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.