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The synthesis and biological activity of the novel series of 1β-methylcarbapenems 1a-f, bearing a variety of 3'',4''-disubstituted pyrrolidinamides as substituents at C-2, are described. Of these carbapenems, diol 1a showed the most potent and well balanced antibacterial activity against Gram-positive and Gram-negative. 1a was also evaluated for pharmacokinetics and in vivo therapeutic efficacy in systemic infections.