Activity-directed synthesis of bioactive small molecules
Lead Research Organisation:
University of Leeds
Department Name: Sch of Chemistry
Abstract
Activity-directed synthesis (ADS) is a novel discovery approach that we have developed in which novel bioactive small molecules emerge in parallel with associated syntheses. Distinctively, ADS harnesses the promiscuity of reactions that can yield alternative products. The project will involve the expansion of the platform of chemical reactions that are configured for activity-directed synthesis (ADS), and the exploitation of ADS in the discovery of novel and diverse small molecules with specific biological functions.
Organisations
Studentship Projects
| Project Reference | Relationship | Related To | Start | End | Student Name |
|---|---|---|---|---|---|
| EP/N509681/1 | 01/10/2016 | 30/09/2021 | |||
| 1939663 | Studentship | EP/N509681/1 | 01/10/2017 | 30/09/2021 | Abbie Leggott |
| Description | Activity-directed synthesis was shown to be a feasible approach to drive antibacterial discovery. An array of 220 Pd-catalysed microscale reactions was executed, and the crude products were evaluated for activity against the ATCC 29213 strain of S. aureus. Scale-up of the hit reactions, purification and evaluation, enabled expansion of the structure activity relationship of a series of quinazolinones. |
| Exploitation Route | The outcomes of my project could inform other activity-directed synthesis projects within my research group. |
| Sectors | Chemicals,Pharmaceuticals and Medical Biotechnology |