Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376555 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated in 14, which is a potent thrombin inhibitor (Ki = 1.2 nM) that exhibits robust efficacy in canine anticoagulation and thrombosis models upon oral administration.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kevin D. Kreutter, Tianbao Lu, Lily Lee, Edward C. Giardino, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald, Barbara J. Haertlein, Venkatraman Mohan, Carl Crysler, Stephen Eisennagel, Malini Dasgupta, Martin McMillan, John C. Spurlino,