Novel Potent and Selective Thrombin Inhibitors Based on a Central 1,4-Benzoxazin-3(4H)-one Scaffold.
[摘要]:scaffold, benzamidine P1 arginine side chain mimetic and various P3 moieties are described. The most potent compd. (I) in the series, exhibited a Ki of 2.6 nM in vitro for thrombin and high selectivity against trypsin and factor Xa.
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