Modification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen
dc.authorid | AY, Mehmet/0000-0002-1095-1614 | |
dc.authorid | Gungor, Tugba/0000-0001-5261-1856 | |
dc.authorid | Celik, Ayhan/0000-0003-1355-9252 | |
dc.contributor.author | Celik, Ayhan | |
dc.contributor.author | Yetis, Gulden | |
dc.contributor.author | Ay, Mehmet | |
dc.contributor.author | Gungor, Tugba | |
dc.date.accessioned | 2025-01-27T20:14:34Z | |
dc.date.available | 2025-01-27T20:14:34Z | |
dc.date.issued | 2016 | |
dc.department | Çanakkale Onsekiz Mart Üniversitesi | |
dc.description.abstract | The 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.sponsorship | Scientific and Technological Research Council of Turkey (TUBITAK) [110T754, 113Z706] | |
dc.description.sponsorship | This 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.doi | 10.1016/j.bmcl.2016.06.081 | |
dc.identifier.endpage | 4060 | |
dc.identifier.issn | 0960-894X | |
dc.identifier.issn | 1464-3405 | |
dc.identifier.issue | 16 | |
dc.identifier.pmid | 27390065 | |
dc.identifier.scopus | 2-s2.0-84977110595 | |
dc.identifier.scopusquality | Q2 | |
dc.identifier.startpage | 4057 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmcl.2016.06.081 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12428/21135 | |
dc.identifier.volume | 26 | |
dc.identifier.wos | WOS:000380574400041 | |
dc.identifier.wosquality | Q2 | |
dc.indekslendigikaynak | Web of Science | |
dc.indekslendigikaynak | Scopus | |
dc.indekslendigikaynak | PubMed | |
dc.language.iso | en | |
dc.publisher | Pergamon-Elsevier Science Ltd | |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry Letters | |
dc.relation.publicationcategory | info:eu-repo/semantics/openAccess | |
dc.rights | info:eu-repo/semantics/closedAccess | |
dc.snmz | KA_WoS_20250125 | |
dc.subject | Nitroreductase | |
dc.subject | Prodrugs | |
dc.subject | Sulfamethoxazole | |
dc.title | Modification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen | |
dc.type | Article |