ACS Chemical Neuroscience · 2020 · 12 citations · 34 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryNeuropharmacologyStructure-activity RelationshipsNeurodegenerative Disease PharmacologyNeurodegenerative DiseasesParkinson DiseaseProtein AggregationProtein Aggregation DisordersStructure-activity Relationship AnalysisAggregation InhibitorsAlpha-synuclein AggregationAlpha-synuclein MisfoldingAlpha-synuclein-targeted TherapyProtein AggregatesProtein Aggregation InhibitionProtein Aggregation InhibitorsStructure - Activity Relationship Optimization
A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesized and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation in vitro. The compounds were found to inhibit α-syn aggregation with efficacy comparable to the promising drug candidate anle138b. The results of this study indicate that compounds 8b, 8l, and 9f may qualify as secondary leads for the structure–activity relationship studies aimed to identify the suitable compounds for improving the modulatory activity targeted at α-syn self-assembly related to Parkinson’s disease.
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