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Saturated bioisosteres of benzene and their application in drug design

Project description

Novel saturated benzene bioisosteres developed

Modern medicinal chemistry exploits only a limited chemical space, with most drugs that target proteins consisting of phenyl-containing organic molecules. Although safe compounds can be identified outside conventional drug chemistry, the chemical synthesis methodology for delivering novel compounds is limited. The EU-funded BENOVELTY project will synthesise novel saturated bioisosteres of benzene rings. Scientists will incorporate these structures into known anti-inflammatory, antiviral and antihypertensive drugs instead of the fragment of the benzene ring. The key objective is to expand the drug chemical space and generate patent-free analogues with improved physicochemical and biological properties.

Objective

More than 500 of all existing drugs are phenyl-containing organic molecules. During the recent years, however, pharmaceutical companies struggle to deliver novel drugs to the market, because of the lack of innovative practical approaches towards novel drug-like “chemical space.” In this project, we will address this issue by developing novel saturated bioisosteres for ortho- and meta-substituted benzenes, and incorporate them into several known drugs (intiinflamatory Aceclofenac, antiviral Tipranavir, antihypertensive Oxprenolol, etc) to provide novel patent-free analogues with improved physico-chemical and biological properties.

Keywords

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Programme(s)

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Topic(s)

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Funding Scheme

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ERC-COG - Consolidator Grant

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Call for proposal

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(opens in new window) ERC-2020-COG

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Host institution

ENAMINE LIMITED LIABILITY COMPANY,RESEARCH AND PRODUCTION ENTERPRISE
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 1 997 500,00
Address
78 WINSTON CHURCHILL STR
02094 KYIV
Ukraine

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SME

The organization defined itself as SME (small and medium-sized enterprise) at the time the Grant Agreement was signed.

Yes
Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
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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.

€ 1 997 500,00

Beneficiaries (1)

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