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New weapons in fight against superbug
18 August 2006
Antibacterial compounds, active against the life-threatening superbug MRSA, have been made by UK scientists.
As MRSA (methicillin resistant Staphylococcus aureus) becomes increasingly resistant to commonly used antibiotics, the search for new types of antibiotics to combat the infection is ever more urgent.
David Spring and colleagues at the University of Cambridge, in collaboration with researchers the pharmaceutical companies AstraZeneca, Alderley Park, and Pfizer, Sandwich, used a technique called diversity-oriented synthesis to make a wide range of structurally diverse compounds, some of which have antibacterial activity against MRSA.
- Mark Ladlow
'Structurally diverse compound collections are essential for discovering novel pharmacologically active small molecules. Historically, natural product extracts were the source of small molecules,' said Spring. However, he added, there are significant disadvantages with this approach, such as limited availability of the natural product and difficulty in making synthetic analogues.
Spring and colleagues started their synthesis with a series of simple two-carbon molecules (based on diazoacetate). Three different reactions were carried out on each starting material, with further divergent reaction pathways being followed after that, to generate complexity. The team ended up with 223 molecules with unique structural features. About two percent of these molecules were found to be active against MRSA.
Superbug: common antibacterial drugs can't kill off MRSA (above)
The active compounds discovered by Spring and colleages are being followed up by co-workers at Addenbrooke's Hospital, Cambridge, UK, and the University of Cambridge to investigate the scope of their activity and to understand their mode of action.
E E Wyatt, S Fergus, W R J D Galloway, A Bender, D J Fox, A T Plowright, A S Jessiman and D R Spring, Chem. Commun., 2006