A new series of 1 beta-methyl carbapenems, in which a disubstituted-am
inothiocarbonylthio moiety was attached to the C-2 position of the car
bapenem nucleus, were prepared and evaluated for anti-MRSA activity. T
hese derivatives showed good in vitro antibacterial activity against h
igh-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. (C) 1998 Elsevie
r Science Ltd. All rights reserved.