PMID: 
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Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G,
Liu Z,
Wang X,
Lu T,
DesJarlais RL,
Thieu T,
Zhang J,
Devine ZH,
Du F,
Li Q,
Milligan CM,
Shaffer P,
Cedervall PE,
Spurlino JC,
Stratton CF,
Pietrak B,
Szewczuk LM,
Wong V,
Steele RA,
Bruinzeel W,
Chintala M,
Silva J,
Gaul MD,
Macielag MJ,
Nargund R
J Med Chem (2022)
Abstract
Activated factor XI (FXIa) inhibitors are promising novel anticoagulants with low bleeding risk compared with current anticoagulants. The discovery of potent FXIa inhibitors with good oral bioavailability has been challenging. Herein, we describe our discovery effort, utilizing nonclassical interactions to improve potency, cellular permeability, and oral bioavailability by enhancing the binding while reducing polar atoms. Beginning with literature-inspired pyridine N-oxide-based FXIa inhibitor
We are not aware of any publication which cites or mentions this structure.