Objective
Resistance to antibiotics is a major concern worldwide and has led to an urgent need to identify antibacterial agents with modes of action distinct from the established classes. The antibacterial natural product pleuromutilin is such a candidate and has been the focus of biological and medicinal studies in recent years. Unfortunately, pleuromutilin has poor pharmacokinetic properties and the compound is readily metabolised by enzymes. Although the natural product itself is not a very good drug, analogues of pleuromutilin look promising. This project will provide access to analogues of the natural product with drug–like properties that cannot currently be prepared, thus paving the way for new therapeutics based on the pleuromutilin scaffold that will improve the quality of life of people in the European Community We will develop new stereoselective processes in which the sequencing of a number of individual chemical reactions allows access to a complex, cyclic system in one synthetic step, using one reagent. We will assemble the skeleton of the antibacterial, pleuromutilin using the lanthanide reagent SmI2 to orchestrate the reaction sequencing so that we get a high yield while achieving good control over the stereochemistry of the product. Our proposal is that different parts of a molecule will react one after the other in an ordered sense, like toppling dominos, until a pleuromutilin–like product is reached. The results of our work will be of interest to synthetic chemists working in academic and industrial laboratories in Europe and throughout the world. The specific objectives of the multidisciplinary project are: - to investigate the individual reaction steps of the proposed sequence using model compounds. - to develop reaction sequencing in a concise synthesis of the tricyclic core of pleuromutilin. - to develop the first asymmetric route to pleuromutilin. - to prepare analogues of pleuromutilin and to carry out their preliminary biological evaluation.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- medical and health sciences basic medicine pharmacology and pharmacy pharmaceutical drugs antibiotics
- natural sciences biological sciences biochemistry biomolecules proteins enzymes
- natural sciences chemical sciences
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Topic(s)
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
FP7-PEOPLE-2007-2-1-IEF
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Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Coordinator
M13 9PL Manchester
United Kingdom
The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.