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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Tarih

2016

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Pergamon-Elsevier Science Ltd

Erişim Hakkı

info:eu-repo/semantics/closedAccess

Özet

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.

Açıklama

Anahtar Kelimeler

Nitroreductase, Prodrugs, Sulfamethoxazole

Kaynak

Bioorganic & Medicinal Chemistry Letters

WoS Q Değeri

Q2

Scopus Q Değeri

Q2

Cilt

26

Sayı

16

Künye