#$%^&*AU2018227936A120180927.pdf#####ABSTRACT NIH 0 NH HN 0 N N I. Amid linkage H Hu- R R R 1l. Unsubstituted metal binding enterobachn I triscatecholate sideropohre 2 (R= H or Ac) oran Trarsaportdiated Dug D9eivery C IiV ~)OI~t dd(~II~ Am#001Ad snd AmaxkUiln Affdn~p@WrIJIn Cooqiupaieo Ahfi'psuadomomi V10,f 00 MRl And-psadimww KMCm4O54JO p Figure 1 An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against P. aeruginosa. The conjugates appear to be assimilated by an induced bacterial iron transport process as their activities were inversely related to iron concentration. The easily synthesized triscatecolate siderophores can be used with a variety of drugs as conjugates to target antibiotic-resistant Gram-negative bacteria.
