Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors

[Display omitted] 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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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 28; no. 6; pp. 987 - 992
Main 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.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.04.2018
Elsevier
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Factor XIa inhibitors
FXIa
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Pyridazine
Pyridazinone
Science & Technology
Thrombosis
Pyridazinone
FXIa
Thrombosis
Pyridazine
Factor XIa inhibitors
COAGULATION-FACTOR XIA
PYRIDINE
OLIGONUCLEOTIDE
PREVENTION
RISK
DISCOVERY
DEFICIENCY
THROMBUS PROPAGATION
REDUCED INCIDENCE
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Summary:[Display omitted] 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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2018.02.049