Structure-based design of novel potent nonpeptide thrombin inhibitors

…, H Nar, H Priepke, U Ries, JM Stassen…

Index: Hauel, Norbert H.; Nar, Herbert; Priepke, Henning; Ries, Uwe; Stassen, Jean-Marie; Wienen, Wolfgang Journal of Medicinal Chemistry, 2002 , vol. 45, # 9 p. 1757 - 1766

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Citation Number: 388

Abstract

The clinical syndromes of thromboembolism are evoked by an excessive stimulation of the coagulation cascade. In this context, the serine protease thrombin plays a key role. Considerable efforts have therefore been devoted to the discovery of safe, orally active inhibitors of this enzyme. On the basis of the X-ray crystal structure of the peptidelike thrombin inhibitor NAPAP complexed with bovine thrombin, we have designed a new ...