哒嗪和哒嗪酮衍生物作为强效且选择性的凝血因子XIa抑制剂。
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
作者信息
Hu Zilun, Wang Cailan, Han Wei, Rossi Karen A, Bozarth Jeffrey M, Wu Yiming, Sheriff Steven, Myers Joseph E, Luettgen Joseph M, Seiffert Dietmar A, Wexler Ruth R, Quan Mimi L
机构信息
Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540, United States.
Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540, United States.
出版信息
Bioorg Med Chem Lett. 2018 Apr 1;28(6):987-992. doi: 10.1016/j.bmcl.2018.02.049. Epub 2018 Feb 27.
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.
哒嗪和哒嗪酮衍生物被设计并合成为凝血因子XIa抑制剂。发现了对因子XIa具有个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适度的口服生物利用度。
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