Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol O-Methyltransferase.
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DOI: 10.1021/acs.jmedchem.8b01126
Abstract: A series of 8-hydroxy quinolines were identified as potent inhibitors of catechol O-methyltransferase (COMT) with selectivity for the membrane-bound form of the enzyme. Small substituents at the 7-position of the quinoline were found to increase… read more here.
Keywords: hydroxyquinolines inhibitors; optimization hydroxyquinolines; inhibitors catechol; catechol methyltransferase ... See more keywords
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol O-Methyltransferase
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DOI: 10.1021/acsmedchemlett.9b00345
Abstract: A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic nitrogen of the core scaffold gave the most potent inhibitors within this series. Rat… read more here.
Keywords: evaluation bicyclic; inhibitors catechol; catechol methyltransferase; bicyclic hydroxypyridones ... See more keywords