Two novel prodrugs of amoxicillin and cephalexin (amoxicillin ProD 1
and cephalexin ProD 1, respectively) were designed and synthesized to
improve the stability and bitter sensation of their parent drugs. The in
vitro susceptibility for both prodrugs was determined against
Escherichia coli, staphylococcus epidermidis, staphylococcus aureus,
Klebsiella pneumonia, streptococcus group A and streptococcus group
B, and was compared to that of their active parent drugs.The
antibacterial screening demonstrates that amoxicillin ProD 1 and
cephalexin ProD 1 were found to be active and are considered among a
small number of prodrugs that have therapeutic activity themselves
before undergoing interconversion via enzymatic or chemical reaction
to their corresponding active parent drugs. Both prodrugs exhibit their
antibacterial activity against different types of bacterial strains due to the presence of β-
lactam ring in their structures. In addition, it is expected that these novel prodrugs will be
much more stable in aqueous media than their corresponding active parent drugs due to the
fact that the chemically sensitive amine group contained in the active parent drug structures is
replaced with an amide, more chemically stable group, in the corresponding prodrugs
