Modification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen

Celik, AyhanYetis, GuldenAy, MehmetGungor, Tugba2025-01-272025-01-2720160960-894X1464-3405https://doi.org/10.1016/j.bmcl.2016.06.081https://hdl.handle.net/20.500.12428/21135The use of existing antibiotics in the form of prodrug followed by activation using enzymes of pathogenic origin could be a useful approach for antimicrobial therapy. To investigate this idea, a common antibiotic, sulfamethoxazole has been redesigned in the form of a prodrug by simple functional group replacement. Upon reductive activation by a type I nitroreductase from a pathogen, the drug displayed enhanced antimicrobial capacity. This strategy could improve the efficacy and selectively of antibiotics and reduce the incidence of resistance. (C) 2016 Elsevier Ltd. All rights reserved.eninfo:eu-repo/semantics/closedAccessNitroreductaseProdrugsSulfamethoxazoleModification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogenArticle26164057406010.1016/j.bmcl.2016.06.081Q2WOS:0003805744000412-s2.0-8497711059527390065Q2