The invention relates to D-Ala-D-Ala ligase inhibitors having the formula:wherein R1 is NH2; R2 is NH2; R3 is selected from
hydrogen,
alkyl, amino, hydroxy, alkoxy, and alkylamino; and R4 and R4′ are each independently
hydrogen or a substituted or unsubstituted, linear, branched, or cyclic,
alkyl, alkenyl, alkynyl,
aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or
hydrogen atoms may be substituted by a
substituent selected from amino, alkylamino, hydroxyl, alkoxyl,
thio,
halogen, nitro, and carbonyl; wherein NR4R4′ incorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy,
halogen,
alkyl, and alkylene, and wherein said naphthyl group in NR4R4′ is bonded to N through a substituted or unsubstituted alkylene
moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway
enzyme in bacterial
cell-wall synthesis, and are suitable for various antibacterial uses.