Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.

Zilun Hu,Cailan Wang,Wei Han,Karen A Rossi,Jeffrey M Bozarth,Yiming Wu,Steven Sheriff,Joseph E Myers,Joseph M Luettgen,Dietmar A Seiffert,Ruth R Wexler,Mimi L Quan

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

Pyridazine and pyridazinone derivatives were designed and synthesized as coagulation factor XIa inhibitors. Potent and selective inhibitors with single digit nanomolar affinity for factor XIa were discovered. Selected inhibitors demonstrated moderate oral bioavailability.

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关键词

Factor XIa inhibitors,FXIa,Thrombosis,Pyridazine,Pyridazinone

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