Bioorganic & Medicinal Chemistry Letters 28 (2018) 1011–1019 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Design, synthesis, and in vitro evaluation of quinolinyl analogues for a-synuclein aggregation a b a a b a c Xuyi Yue , Dhruva D. Dhavale , Junfeng Li , Zonghua Luo , Jialu Liu , Hao Yang , Robert H. Mach , b a,⇑ Paul T. Kotzbauer , Zhude Tu Department of Radiology, Washington University School of Medicine, St Louis, MO, United States Department of Neurology, Washington University School of Medicine, St Louis, MO, United States Department of Radiology, University of Pennsylvania, Perelman School of Medicine, Philadelphia, PA, United States article i nfo abstract Article history: Here we report the synthesis and in vitro evaluation of 25 new quinolinyl analogues for a-synuclein Received 6 January 2018 aggregates. Three lead compounds were subsequently labeled with carbon-11 or ﬂuorine-18 to directly Revised 9 February 2018 assess their potency in a direct radioactive competitive binding assay ng both a-synuclein ﬁbrils and tis- Accepted 14 February 2018 sue homogenates from Alzheimer’s disease (AD) cases. The modest binding afﬁnities of these three radi- Available online 16 February 2018 oligands toward a-synuclein were comparable
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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