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Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-02-27 , DOI: 10.1016/j.bmcl.2018.02.049
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

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.



中文翻译:

哒嗪和哒嗪酮衍生物可作为有效的和选择性的XIa抑制剂

设计并合成了哒嗪和哒嗪酮衍生物作为凝血因子XIa抑制剂。已发现对因子XIa具有一位数纳摩尔亲和力的强效和选择性抑制剂。选定的抑制剂表现出中等的口服生物利用度。

更新日期:2018-02-27
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