Methodology for, and Synthesis of Biologically Active Pyrrolidinone Natural Products.

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Five-membered ring compounds with contain one nitrogen atom, are ubiquitous structural units present on thousands of natural products, in numerous brand-name drugs and agrochemicals, and are widely used to modify catalysts for a particular purpose. These nitrogen "heterocycles" are present in a family of highly complex natural products which exhibit antitumour and antibiotic activity. The search for new antibiotics is particularly important now we are in the "post-penicillin" era and our entering the era when even resistance to antibiotics such as vancomycin is regularly encountered. The search for new antibiotics with different modes of action is an important challenge facing academia and the pharmaceutical industry. The aim of our work is to develop new and efficient methods for the synthesis of nitrogen heterocycles which will have particular application to the synthesis of these antitumour antibiotics. A major part of the project will involve using the developed methodologies to synthesise one of the natural products and, importantly, to prepare simplified analogues. The simplified analogues will be tested for both antibiotic and antitumour activity. In the long term, this research may have an impact on the discovery of new antibiotics and antitumour agents. Moreover, the developed methodologies will have application in the synthesis of a whole range of other biologically important natural products and small molecules.