Synthesis Of Novel Macrocyclic Compounds Derived From Ceftriaxone

Macrocyclization can help improve pharmacological activity, metabolic stability, cell permeability and oral absorption to create better drug candidates. For example, enhancing the oral absorption of the compounds can allow a change in administration route. We tried to improve the oral bioavailability of ceftriaxone, a third-generation cephalosporin having a unique side chain with a 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-astriazin-3-yl group at the C-3 position of the cephem nucleus. We prepared novel macrocycles of ceftriaxone by valuable synthetic methods and confirmed their oral bioavailabilities.