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. 2001 Feb 12;11(3):287-90.
doi: 10.1016/s0960-894x(00)00636-3.

Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors

B Bachand  1 , M Tarazi, Y St-Denis, J J Edmunds, P D Winocour, L Leblond, M A Siddiqui
Affiliations

Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors

B Bachand et al. Bioorg Med Chem Lett. .

Abstract

Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model.

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