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-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 26 Sayı: 16
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1016/j.bmcl.2016.06.081
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.4057-4060
  • Anahtar Kelimeler: Nitroreductase, Prodrugs, Sulfamethoxazole, ARYLAMINE N-ACETYLTRANSFERASES, LOCALIZED PROSTATE-CANCER, DRUG-METABOLISM, CLINICAL-TRIAL, THERAPY
  • Çanakkale Onsekiz Mart Üniversitesi Adresli: Evet

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.