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Small Bicyclic Amines: Unexplored Motifs for Drug Discovery

   Faculty of Engineering and Physical Sciences

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  Prof S Marsden, Dr B Nguyen  No more applications being accepted  Competition Funded PhD Project (Students Worldwide)

About the Project

Small bicyclic amines (SBAs) are introduced as new motifs for drug discovery. The unique bonding arrangements in SBAs means that, on conjugation to (hetero)aromatic rings, the nitrogen remains pyramidalised, in contrast to the planarisation usually observed. This has implications not only for exploration of novel growth vectors but also the physicochemical/pharmacodynamic properties of the molecules: preliminary results show beneficial impact upon basicity, aqueous solubility, logD and metabolic stability. Within the project, we will: (a) develop efficient synthetic routes to SBAs and derivatives; (b) use HTE to identify methods for their arylation in array format; (c) characterise the drug relevant properties of arylated SBAs, and apply machine-learning to the prediction/understanding of these properties; and (d) demonstrate the potential of SBAs in the context of bioactive discovery programmes.

Funding Notes

A highly competitive EPSRC Faculty Doctoral Training Partnership Studentship in collaboration with GlaxoSmithKline, consisting of the award of fees with a maintenance grant of £16,062 for session 2022/23 for 3.5 years. This opportunity is open to all applicants. All candidates will be placed into the EPSRC Faculty Doctoral Training Partnership Studentship Competition and selection is based on academic merit.

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