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Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors

…, JM Di Muzio-Mower, M Juliano, JA Krueger…

文献索引:Coburn, Craig A.; Rush, Diane M.; Williams, Peter D.; Homnick, Carl; Lyle, Elizabeth A.; Lewis, S. Dale; Lucas Jr., Bobby J.; Di Muzio-Mower, Jillian M.; Juliano, Marylou; Krueger, Julie A.; Vastag, Kari; Chen, I-Wu; Vacca, Joseph P. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 10 p. 1069 - 1072

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被引用次数: 26

摘要

Thrombus formation is the culmination of a series of enzymatic reactions in which the serine protease thrombin plays an essential and multifaceted role. For example, thrombin acts directly to promote clot formation by catalyzing the hydrolysis of the soluble plasma protein fibrinogen to insoluble fibrin. Thrombin is also a potent stimulator of platelet aggregation and is required for the biosynthesis of other coagulation factors. Defects in the balance between these ...