Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

Juan Pablo Maianti, Stephen Hanessian

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Vast numbers of prevalent aminoglycoside-modifying enzymes undermine the clinical use of aminoglycoside antibiotics. We present the design and synthesis of a potent broad-spectrum bactericidal aminoglycoside based on available X-ray co-crystal structures within the ribosomal binding-site. The resulting antibiotic displays broad protection of its functional groups from inactivation by clinically relevant resistance enzymes.

Original languageEnglish (US)
Pages (from-to)170-176
Number of pages7
JournalMedChemComm
Volume7
Issue number1
DOIs
StatePublished - 2016
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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