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ChemInform Abstract: Potent and Selective Bicyclic Lactam Inhibitors of Thrombin. Part 4. Transition State Inhibitors.
First published: 27 May 2010
Abstract
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ChemInform Abstract
A variety of bicyclic piperazinone based thrombin inhibitors (VI) (11 examples) are synthesized and evaluated for their activity in vitro and in vivo. These inhibitors display high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in an arterial thrombosis model.
