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Content archived on 2022-12-23

Computer-assisted combinational design, synthesis and testing of new cognition enhancers, anxyolitics and anticonvulsants

Objective

To discover new therapeutics an innovative theoretical computer-assisted approach is developed and validated experimentally in a search for new cognition enhancers, anxiolytics and anticonvulsants. Probability to find new chemical entities are increased by virtual combinatorial design of compounds highly diversed chemically including different types of heterocycles: 5-membered (thiophenes, thiazoles, imidazoles, oxazoles, pyrroles), 6-membered (pyridines, pyrimidines), 7-membered (diazepines, triazepines), fused 5+6-membered heterocycles (indoles, benzothiazoles, purines, indolizines, neutral, mesoionic and cationic azolopyridines). Three supplementary computer-aided methods to drug discovery are used to provide the complex criteria applied to new pharmaceutical leads:
(1) prediction of biological activity spectra;
(2) optimization of leads' properies using artificial neural networks;
(3) prediction of bioavailability and toxicity.

New compounds from different chemical classes are virtually designed, synthesized and tested as potential cognition disorders, anxiolytics and anticonvulsants. Analytical computer system for de novo design of compounds with required complex of properties is developed and applied to the second generation of lead compounds, taking into account the results of the previous experiments and using lead optimisation methods by neural networks and genetic algorithm. The most prospective compounds are selected, synthesized and tested. The innovative approach developed within the frame of the project can be applied for compounds from the other chemical series and in search for new leads in different pharmacotherapeutic areas.

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Programme(s)

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Topic(s)

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Call for proposal

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Funding Scheme

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Coordinator

Aristotelian University of Thessaloniki
EU contribution
No data
Address

54006 Thessaloniki
Greece

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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

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Participants (9)

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