Chapter 9. Anticoagulants: Thrombin and Factor Xa Inhibitors

作者: John M. Fevig , Ruth R. Wexler

DOI: 10.1016/S0065-7743(08)60571-0

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摘要: Publisher Summary This chapter describes anticoagulants with a particular emphasis on thrombin and Xa inhibitors. Thrombin, serine protease of the trypsin family, plays central role in thrombosis haemostasis. It is terminal enzyme coagulation cascade directly responsible for cleavage fibrinogen, resulting precipitation insoluble fibrin, primary component blood clot or thrombus. In addition, key to activation platelets which stimulates aggregation. The development selective, orally active, low molecular weight inhibitors has been an intense research focus search new large number pharmaceutical laboratories. presents overview naturally occurring explains electrophilic transition state Non-covalent based argatroban NAPAP TAPAP are elaborated, non-covalent derived from peptidomimetics discussed. Nonpeptide described. Factor reviewed synthetic pentasaccharides analyzed. An transitions presented. Details monobasic provided discussion less basic also

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