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Design, synthesis and biological evaluation of new selective 5ht7, agonists using combinatorial chemistry, automated organic synthesis and molecular modelling

Objective



Research objectives and content
Our main objective is the design and synthesis of selective 5TH7 agonists. A selective 5TH7, agonist will be very valuable to investigate de effects of 5TH7 receptor stimulation and to provide biological verification methods, both in vivo and in vitro for investigation of 5TH7, antagonists that could be used as psychoactive drugs in psychiatric disorders like depression, anxiety or schizophrenia.
The project includes the following points: - Design of potential selective 5TH7 agonists libraries using the Chem-X molecular modelling suite. - Synthesis of the designed compounds (between 300 and 800 molecules) using combinatorial chemistry and automated organic synthesis techniques. - Test the synthesised libraries as 5HT7 agonists. - Successful ligands will be subjected to a modified Irwin behavioural screen in order to identify SELECTIVE 5HT7 agonists. - Full receptor binding scans of the most promising molecules and evaluation of their in vivo activity.By using combinatorial chemistry and automated synthesis we will synthesise a huge number of molecules that increase the probability of success with lower costs.
Training content (objective, benefit and expected impact)
My main training objective as a medicinal chemist is to learn combinatorial chemistry and automated organic synthesis. Both methodologies are very important in pharmaceutical, agrochemical and biotechnology industries to reduce the time and costs associated with producing effective, marketable and competitive new drugs. I will also develop my knowledge in molecular modelling using the Chem-X molecular modelling suite.
Links with industry / industrial relevance (22) Although the project has no links with industries, the results obtained could be used by pharmaceutical industries in order to develop new psychoactive drugs.

Funding Scheme

RGI - Research grants (individual fellowships)
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Coordinator

UNIVERSITY OF ASTON
Address
Aston Triangle
B4 7ET Birmingham
United Kingdom