Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 16, Pages 7206-7212Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00918
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Funding
- Fundacao para a Ciencia e Tecnologia (FCT) [QUI/U10081/2013, POCI-01-0145-FEDER-006980]
- FCT
- POPH
- FEDER/COMPETE
- COST action [CA15135]
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Because of the lack of significant disease-modifying drugs for neurodegenerative disorders, a pressing need for new chemical entities endowed with IMAO-B still exists. Within this framework, and for the first time, a study was performed to compare coumarin- and chomone-3-phenylcarboxamide scaffolds. Compounds 10a and 10b were the most potent, selective, and reversible noncompetitive IMAO-B. The benzopyrone sp(2) oxygen atom was found to be position independent and a productive contributor for the ligand-enzyme complex stability.
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