A new series of carbapenems, in which disubstituted-aminothiocarbonylthio moiety, directly attached to the C-2 position, were prepared and evaluated for their antibacterial potency. These analogs showed potent activity against high-level MRSA. Among them, 9e and 9i were found to exhibit good in vivo efficacy comparable to that of vancomycin, for mouse septicemia model with high-level MRSA.