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Design, Synthesis and In Vitro Biological Evaluation of 3- styrylbenzimidamides as Potential BACE1 Inhibitors

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A series of 3-styrylbenzimidamides were synthesized and biologically evaluated in a cell free FRET assay as potential BACE1 inhibitors. Some of the synthesized analogues were discovered to have moderate BACE1 inhibitory activities with IC50 values ranging from 9.3 to 295.8 μM. Molecular docking study proposed that the most potent compound (E)-2d bound to BACE1 differently in S3-S2' subpockets forming no polar interaction with the catalytic Asp dyad compared with the 3-styrylbenzimidamides. The results would contribute to the further optimizations on benzimidamide scaffold to achieve novel small molecular BACE1 inhibitors with improved potencies.

Keywords: 3-styrylbenzimidamide; Alzheimer's disease; BACE1 inhibitors; CADD

Document Type: Research Article

Publication date: May 1, 2013

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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