Ohtake N, Imamura H, Jona H, Kiyonaga H, Shimizu A, Moriya M, Sato H, Nakano M, Ushijima R, Nakagawa S
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
Bioorg Med Chem. 1998 Jul;6(7):1089-101. doi: 10.1016/s0968-0896(98)00069-8.
A new series of 1beta-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.
