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

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dc.authoridAY, Mehmet/0000-0002-1095-1614
dc.authoridGungor, Tugba/0000-0001-5261-1856
dc.authoridCelik, Ayhan/0000-0003-1355-9252
dc.contributor.authorCelik, Ayhan
dc.contributor.authorYetis, Gulden
dc.contributor.authorAy, Mehmet
dc.contributor.authorGungor, Tugba
dc.date.accessioned2025-01-27T20:14:34Z
dc.date.available2025-01-27T20:14:34Z
dc.date.issued2016
dc.departmentÇanakkale Onsekiz Mart Üniversitesi
dc.description.abstractThe 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.
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [110T754, 113Z706]
dc.description.sponsorshipThis work was supported by The Scientific and Technological Research Council of Turkey (TUBITAK, Grant Nos. 110T754 & 113Z706). We would like to thank Dr. Gareth A. Roberts (University of Edinburgh, UK) for his critical reading of this manuscript and his comments.
dc.identifier.doi10.1016/j.bmcl.2016.06.081
dc.identifier.endpage4060
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.issue16
dc.identifier.pmid27390065
dc.identifier.scopus2-s2.0-84977110595
dc.identifier.scopusqualityQ2
dc.identifier.startpage4057
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2016.06.081
dc.identifier.urihttps://hdl.handle.net/20.500.12428/21135
dc.identifier.volume26
dc.identifier.wosWOS:000380574400041
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.ispartofBioorganic & Medicinal Chemistry Letters
dc.relation.publicationcategoryinfo:eu-repo/semantics/openAccess
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WoS_20250125
dc.subjectNitroreductase
dc.subjectProdrugs
dc.subjectSulfamethoxazole
dc.titleModification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen
dc.typeArticle

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