Abstract: 

The present invention describes the preparation and respective application of innovative non-nitrocatechol COMT inhibitors, that manifested improved pharmacokinetic and pharmacodynamic properties compared to those currently used in the clinic (e.g. tolcapone, entacapone, opicapone).

Background: 

COMT has been an interesting pharmacological target for adjuvant terapy on Parkison´s disease and other CNS disorders. However, current COMT inhibitors on the therapeutic are associated with problems related to their ADMET properties, namely short half-lives, citotoxicity, and low BBB permeability.

Benefits: 

Selective COMT inhibitors; Suitable lipophilicity for BBB permeability; Less cytotoxic than standard COMT inhibitors.

Potential comercial use/applications: 

Co-adjuvant drugs for treatment of Parkinson´s disease; Therapeutic agents for other neuropsychiatric disorders associated with low dopamine levels.

Owners: 
University of Porto