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Details of Grant 

EPSRC Reference: GR/T20380/01
Title: Total Synthesis & Biological Mode of Action of New Antibiotic Structural Motifs
Principal Investigator: Moloney, Professor M
Other Investigators:
Researcher Co-Investigators:
Project Partners:
Department: Oxford Chemistry
Organisation: University of Oxford
Scheme: Standard Research (Pre-FEC)
Starts: 30 March 2005 Ends: 29 June 2008 Value (£): 219,733
EPSRC Research Topic Classifications:
Biological & Medicinal Chem. Chemical Synthetic Methodology
Drug Formulation & Delivery
EPSRC Industrial Sector Classifications:
Pharmaceuticals and Biotechnology
Related Grants:
Panel History:  
Summary on Grant Application Form
The development of resistance of pathogenic bacteria to commonly used antibiotics, and the emergence of viral infections amongst immunocompromised sections of the community, has focussed significant efforts in the identification, design, synthesis and evaluation of new drug leads. There is therefore an urgent need for the identification of new drug candidates, and one important source has always been natural products. Oxazolomycin is the parent member of a class of antibiotics, which are isolated from Streptomyces spp., and exhibit wide ranging and potent antibiotic activity, including inhibitory activity against Gram positive bacteria, antiviral activity against vaccinia, herpes simplex type I, and influenza A, as well as in vivo antibacterial and antitumour activity. Notably, this biological activity is coupled with low toxicity. The synthetic challenge offered by the unusual densely functionalised lactam and the sensitive diene and triene units of these compounds have hitherto precluded effective syntheses of these compounds. We propose (i) to complete a total synthesis of oxazolomycin using methodology which has only recently become available; (ii) to use this route to access analogues; (iii) to evaluate their biological activity; (iv) to investigate the biological mode of action of these analogues.
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Project URL: http://research.chem.ox.ac.uk/mark-moloney.aspx
Further Information:  
Organisation Website: http://www.ox.ac.uk