A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.
Monoamine oxidase B (MAO-B) inhibitors are used to treat Parkinson's disease. In this study, we searched for novel MAO-B inhibitors using a scaffold hopping approach based on our experience with the thiazolidinedione (TZD) class of compounds as MAO-B inhibitors. Several novel compounds were identified, with potencies in the low nanomolar and low micromolar range. We also found that derivatives of the natural product sulfuretin are potent MAO-A and MAO-B inhibitors.
Department of Pharmaceutical Sciences, Northeast Ohio Medical University, 4209 State Route 44, Rootstown, OH 44272, USA. wgeldenh@neomed.edu
Werner J
WJ
Geldenhuys
Max O
MO
Funk
Cornelis J
CJ
Van der Schyf
Richard T
RT
Carroll
D001572:Benzofurans / Q000737:chemistry / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D008995:Monoamine Oxidase / Q000737:chemistry / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship
D001572:Benzofurans; D005419:Flavonoids; D008996:Monoamine Oxidase Inhibitors; D054852:Small Molecule Libraries; D008995:Monoamine Oxidase; C054989:sulfuretin