Routes to 2-aminooxazolines using single and multistep enzymatic transformations
Lead Research Organisation:
University College London
Department Name: Chemistry
Abstract
This project aims to use enoyl reductase and transaminase native enzymes and mutants, together with other chemical or enzymatic steps (as single step or multi-enzyme pathways) to synthesise 2-aminooxazolines. The project will pave the way for the synthesis of such bioactive compounds in a sustainable fashion, cheaply and efficiently by biocatalysis in E. coli or other bacteria, under mild reactions conditions.
Organisations
Studentship Projects
| Project Reference | Relationship | Related To | Start | End | Student Name |
|---|---|---|---|---|---|
| BB/M009513/1 | 01/10/2015 | 31/03/2024 | |||
| 1758915 | Studentship | BB/M009513/1 | 01/10/2016 | 17/06/2021 | Alexandra King |
| Description | With a growing interest in the pharmaceutical, fine chemical and agrochemical industry for environmentally benign and sustainable syntheses, biocatalysis has emerged as a forerunner in the field of green chemistry. Significant advantages over traditional chemical routes have been demonstrated, including high regio- and stereoselectivity under mild, non hazardous conditions, as well as high efficacy and cost-effectiveness. From this award, we have investigated the application of a one-pot enzymatic cascade utilising ene-reductases (ERs) and ?-transaminases (?-TAm) for the molecular assembly of optically-active 2-aminooxazolines employed as TAAR1 inhibitors. These TAAR1 agonists were recently patented for numerous neuropsychiatric disorders including depression, schizophrenia, and Parkinson's disease, amongst others. |
| Exploitation Route | This funding has successfully developed the enzymatic cascade of ene-reductases (ERs) and ?-transaminases (?-TAm) as a cost effective and efficacious strategy for the generation of chiral synthons and bioactive molecules, surpassing many traditional synthetic chemistry approaches. Enantioenriched products afforded from this cascade offer high value chiral building blocks in agrochemical, pharmaceutical and fine chemical applications. |
| Sectors | Agriculture, Food and Drink,Chemicals,Environment,Manufacturing, including Industrial Biotechology,Pharmaceuticals and Medical Biotechnology |
| Description | Research from this award has been pursued with non-academic applications in mind. Findings have been positive, and research is ongoing. Thus, at this current stage potential economic and societal impacts are still being explored. |