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

ÇELİK A., Yetis G., AY M. , GÜNGÖR T.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.26, sa.16, ss.4057-4060, 2016 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 26 Konu: 16
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1016/j.bmcl.2016.06.081
  • Sayfa Sayıları: ss.4057-4060


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.