Cyanamides: Exploring New Approaches Towards Heterocyclic Scaffolds

The development of new medicines are essential to ensure improvement in the health of the world's population, and to tackle unmet medical needs. Furthermore, with the advances in genomic research, it is estimated that several thousand new biological targets associated with medical conditions will soon be identified. This exerts enormous pressure on scientists to design, develop and deliver new molecules in a timely fashion to meet these demands.
Traditionally, the search for new lead molecules in drug discovery has been mainly focused on natural sources or screening existing compound libraries available from the pharmaceutical banks. Unfortunately, these processes could be time consuming as well as hitting dead ends with the relatively limited structural diversity and complexity of molecular scaffolds available.

This project will deliver new chemical methods for the construction of novel molecular cores from a simple, readily available and low cost starting material.

Heterocyles are carbon based ring compounds containing at least one heteroatom (such as oxygen, nitrogen, sulphur) in the ring and, are frequently the essential active component of drugs. The key innovation of this proposal is the invention, development and application of a new set of chemical reagents, called cyanamides. These reagents contain unique chemical linkages with multiple functionality, and are important in performing multiple roles in chemical synthesis. The new chemistry described utilises very mild conditions to deliver arrays of structurally complex and diverse molecules.
The process will lead to the identification of new chemical pathways for the construction of heterocyclic systems, which are key to the drug discovery programme. Furthermore as the protocol involves coupling of two fragments, there is significant scope to explore a wide variety of functional groups that could be introduced directly onto the heterocyclic core of the molecule. This will enable rapid access to diverse molecular frameworks that are not currently represented. This will lead to the generation of potential lead compounds against a wide variety of biological targets. Collaborative research both within University and Industry will help evaluate the new compounds as potential drugs.

The wider outcome of the proposed project will have a positive contribution to science and society in general.

The proposed research into the development of a new synthetic methodologies to novel pharmacophores, will impart influence on: (i) the global 'healthcare sector', by helping to expedite the research into the design, development and timely delivery of new pharmaceutical entities; would influence the (ii) UK based commercial establishment engaged in 'manufacturing and delivering' of chemical entities, building blocks, and therapeutics.
The novel chemistry to access diverse heterocycles will hugely impact the way such compounds are synthesised for various applications e.g. in the field of material and biological sciences. The chemical, pharmaceutical and materials science community, in general, will be the main end users of the technology and, will derive a direct benefit from the studies undertaken in this project.
The project will deliver state-of the art research objectives towards the training of a postdoctoral scientist and, would invest into developing young minds in the field of novel chemical transformations and utilisation of an under-explored chemical entities.

The avenues to novel intellectual property generated from the current research, will be thoroughly assessed with the support of the Research and Enterprise Department at the University of Lincoln.