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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.

Host institution

ENAMINE LIMITED LIABILITY COMPANY,RESEARCH AND PRODUCTION ENTERPRISE
Net EU contribution
€ 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
€ 1 997 500,00

Beneficiaries (1)