Bioorganic & Medicinal Chemistry Letters 28 (2018) 1030–1036 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Design and characterization of bivalent compounds as potential neuroprotectants for Alzheimer’s disease: Impact of the spacer on biological activity Liu He, Ashley Boice, Kai Liu, Xing Yan, Yuqi Jiang, Shijun Zhang Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA ar ti c l e i nf o ab stra ct Article history: In our continuing efforts to develop bivalent compounds as potential neuroprotectants for Alzheimer’s Received 5 January 2018 disease, a series of bivalent compounds that contain cholesterylamine and an extended spacer were syn- Revised 10 February 2018 thesized and biologically characterized. Our results demonstrated that incorporation of a piperazine ring Accepted 13 February 2018 into the spacer composition signiﬁcantly improved the protective potency in MC65 cell models. Our Available online 14 February 2018 results also suggested that the optimal spacer length for such bivalent compounds ranges from 17 to 21 atoms, and further spacer extension beyond 21 atoms results no further optimization. Notably, incor- Keywords: poration of a piperazine ring into the spacer diminished the biometal chelating capacity for these bivalent Alzheimer’s disease compounds, thus
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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