Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.
作者信息
Bachand B, Tarazi M, St-Denis Y, Edmunds J J, Winocour P D, Leblond L, Siddiqui M A
机构信息
BioChem Pharma Inc., Laval, Québec, Canada.
出版信息
Bioorg Med Chem Lett. 2001 Feb 12;11(3):287-90. doi: 10.1016/s0960-894x(00)00636-3.
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.
摘要
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