2024
DOI: 10.1021/jacs.3c14490
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Conjugation to Native and Nonnative Triscatecholate Siderophores Enhances Delivery and Antibacterial Activity of a β-Lactam to Gram-Negative Bacterial Pathogens

Rachel N. Motz,
Chuchu Guo,
Artur Sargun
et al.

Abstract: Developing new antibiotics and delivery strategies is of critical importance for treating infections caused by Gramnegative bacterial pathogens. Hijacking bacterial iron uptake machinery, such as that of the siderophore enterobactin (Ent), represents one promising approach toward these goals. Here, we report a novel Ent-inspired siderophore−antibiotic conjugate (SAC) employing an alternative siderophore moiety as the delivery vector and demonstrate the potency of our SACs harboring the βlactam antibiotic ampic… Show more

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Cited by 9 publications
(2 citation statements)
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“…Nolan continued to be a pioneer in this field, synthesizing nonnative Ent analogs. These synthetically simplified analogs retain activity and still show uptake through the FepA sequence . Furthermore, these EACs were found to have increased activity against a library of ESKAPE pathogens, bacteria typically associated with causing drug-resistant infections .…”
Section: Catecholate and Phenolate Siderophores: Enterobactinmentioning
confidence: 99%
See 1 more Smart Citation
“…Nolan continued to be a pioneer in this field, synthesizing nonnative Ent analogs. These synthetically simplified analogs retain activity and still show uptake through the FepA sequence . Furthermore, these EACs were found to have increased activity against a library of ESKAPE pathogens, bacteria typically associated with causing drug-resistant infections .…”
Section: Catecholate and Phenolate Siderophores: Enterobactinmentioning
confidence: 99%
“…These synthetically simplified analogs retain activity and still show uptake through the FepA sequence . Furthermore, these EACs were found to have increased activity against a library of ESKAPE pathogens, bacteria typically associated with causing drug-resistant infections . Recently, the Nolan lab conjugated enterobactin to cisplatin, a potent anticancer reagent.…”
Section: Catecholate and Phenolate Siderophores: Enterobactinmentioning
confidence: 99%