Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors

Santosh Kumar Adla,Barbora Slavikova,Markéta Šmídková,Eva Tloustova,Martin Svoboda,Vojtech Vyklicky,Barbora Krausova,Pavla Hubalkova,Michaela Nekardova,Kristina Holubova,Karel Vales,Milos Budesinsky,Ladislav Vyklicky,Hana Chodounska,Eva Kudova

Steroids（2017）

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摘要

•Synthesis of new amide-based inhibitors of NMDA receptors.•Strong inhibitors of NMDA currents.•The Caco-2 assay was used to evaluate permeability of new compounds.•Compounds with minimal or no adverse hepatic effect.•Amide-based inhibitors of NMDA receptors are able to cross blood-brain-barrier.

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关键词

Neurosteroid,NMDA receptor,Structure-activity relationship,Amide,Blood-brain-barrier permeability,Caco-2 assay

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