| Autor: |
Guozhang Xu, Zhijie Liu, Xinkang Wang, Tianbao Lu, Renee L. DesJarlais, Tho Thieu, Jing Zhang, Zheng Huang Devine, Fuyong Du, Qiu Li, Cynthia M. Milligan, Paul Shaffer, Peder E. Cedervall, John C. Spurlino, Christopher F. Stratton, Beth Pietrak, Lawrence M. Szewczuk, Victoria Wong, Ruth A. Steele, Wouter Bruinzeel, Madhu Chintala, Jose Silva, Michael D. Gaul, Mark J. Macielag, Ravi Nargund |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 65(15) |
| ISSN: |
1520-4804 |
| Popis: |
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 |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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