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Molecular renovation- chemical disassembly to generate- prefabricated architecture for advanced library generation


The main topic of the project is the molecular renovation ¿ chemical disassembly and reassembly to generate prefabricated architectures for advanced library generation starting from natural products or natural product-like scaffolds. This is an innovative and completely unexploited field. The products produced by living systems have always fascinated and inspired synthetic organic chemists.

As our skills and tools advanced, the compounds chosen for synthesis became ever more challenging. So it is no surprise that today's favourite synthesis targets are found among the most fundamentally complex natural substances ever discovered. The pharmaceutical industry recognizes the complexity of synthesis, but also derives value from natural products as leads for drug candidates.

Unfortunately when natural products are used to derive drugs, it usually takes a long time to synthesize analogues in a given series. Also many of these molecules of high molecular weight usually show interesting biological activity because of their complex scaffolding. Conversely many of the components used to prepare these larger structures often possess some biological function and show specific activity at receptors.

For all these reasons, we would like to investigate the divestment and recombination of macromolecular structures. The combinatorial chemistry concept will be used as systematic approach for the disassembly of these macromolecules, to generate either prefabricated hybrid structures as novel species that demonstrate independent biological activity or as unique scaffolding for further combinatorial decoration.

The ability to use these smaller sub-units to develop new molecular structures, by using the fragments as templates or advanced precursors, would offer a unique level of access to new combinatorial libraries of new drugs and molecules with high biological activity.

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The Old Schools, Trinity Lane
United Kingdom

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