Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors. Issue 6 (1st April 2018)

• Record Type: Journal Article
• Authors: 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.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 6(2018)
• Page Start: 987
• Page End: 992
• Publication Date: 2018-04-01
• Subjects: Factor XIa inhibitors -- FXIa -- Thrombosis -- Pyridazine -- Pyridazinone; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.02.049
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.