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- W2070065625 abstract "The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The arylsulfonamide-valerolactam scaffold was derived based on the proposed bioisosterism to the arylcyanoguanidine-caprolactam core in known FXa inhibitors. The SAR study led to compound 46 as the most potent FXa inhibitor in this series, with an IC(50) of 7 nM and EC(2×PT) of 1.7 μM. The X-ray structure of compound 40 bound to FXa shows that the sulfonamide-valerolactam scaffold anchors the aryl group in the S1 and the novel acylcytisine pharmacophore in the S4 pockets." @default.
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- W2070065625 date "2011-12-01" @default.
- W2070065625 modified "2023-10-16" @default.
- W2070065625 title "Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors" @default.
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- W2070065625 doi "https://doi.org/10.1016/j.bmcl.2011.06.098" @default.
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