Comparative biological properties of some synthetic olivanic acid analogues.

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Abstract
A series of olivanic acid/thienamycin analogs were prepared by total synthesis. Particular attention was given to the effect of the side chain substituents on the chemical, .beta.-lactamase and metabolic stability of the final products. All the compounds possessed a broad and high level of in vitro antibacterial activity against gram-positive and gram-negative organisms, including .beta.-lactamase-producing strains. Two derivatives were selected for further evaluation on the basis of in vitro activity, ease of synthesis and stability parameters. Improved metabolic stability of the selected analogs, relative to the naturally occurring olivanic acid, MM 13902, was demonstrated in terms of better activity, higher blood levels and improved urinary recovery in in vivo studies in mice.