[1] In 1976, fermentation broths obtained from the soil bacterium Streptomyces cattleya were found to be active in a screen for inhibitors of peptidoglycan biosynthesis.

[6] Unlike penicillins, which are rendered ineffective through rapid hydrolysis by the β-lactamase enzyme present in some strains of bacteria, thienamycin remains antimicrobially active.

[citation needed] The hydroxyethyl side chain of thienamycin is thought to be a result of two separate methyl transfers from S-adenosyl methionine.

How the cysteaminyl side-chain is incorporated is largely unknown, although ThnT, ThnR, and ThnH are involved in the processing of CoA to cysteamine for use in the pathway.

[citation needed] Due to low titre and to difficulties in isolating and purifying thienamycin produced by fermentation, total synthesis is the preferred method for commercial production.

The starting β-lactam for the pathway given above can be synthesized using the following method (Figure 4):[12] Since thienamycin decomposes in the presence of water, it is impractical for the clinical treatment of bacterial infections, so stable derivatives were created for medicinal consumption.