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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.

DOI:10.1016/s0960-894x(00)00636-3
PMID:11212093
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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