Poster Presentation 12th Australian Peptide Conference 2017

Hydroxylamine derivatives as new compounds to treat antibiotic bacterial resistance (#207)

Laia Miret Casals 1 , Aida Baelo 2 , Esther Julián 3 , Josep Astola 2 , Ariadna Lobo-Ruiz 1 , Fernando Albericio 1 4 5 , Eduard Torrents 2
  1. Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain
  2. Bacterial Infections and antimicrobial therapies. Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute of Science and Technology, Baldiri Reixac, 15-21, 08028 Barcelona, Spain.
  3. Group of Mycobacteriology. Department of Genetics and Microbiology, Facultat de Biociències, Universitat Autònoma de Barcelona, Bellaterra 08193, Barcelona, Spain.
  4. CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Barcelona, Spain
  5. School of Chemistry & Physics, University of Kwazulu-Natal, Durban 4001, South Africa

Bacterial pathogens have developed mechanisms of resistance to antibiotics, reducing or eliminating drastically the effectiveness of antibacterial drugs. Multi-drug-resistant bacteria causing severe infections mainly grow in complex bacterial communities known as biofilms, which are difficult to reach for antibiotics and immune cells. As drug resistance is becoming a threatening problem, it is necessary to develop new antimicrobial agents with novel mechanisms of action. Here, we synthesized a small library of N-substituted hydroxylamine (N-HA) compounds with antibacterial activity. We demonstrate the broad antimicrobial effect of several drug candidates against a variety of Gram-positive and Gram-negative bacteria by inhibiting the bacterial ribonucleotide reductase (RNR) enzyme, which provides the building blocks for DNA synthesis and repair. Furthermore, the most promising compounds are able to reduce the biomass of an established biofilm on Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coli