期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 10, 页码 2648-2653出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.046
关键词
thrombin inhibitor; anticoagulant; factor IIa inhibitor; serine protease inhibitor; amidine
Synthesis and SAR of orally active thrombin inhibitors of the D-Phe-Pro-Arg type with focus on the P2-moiety are described. The unexpected increase in in vitro potency, oral bioavailability, and in vivo activity of inhibitors with dehydroproline as P2-isostere is discussed. Over a period of 24 h the antithrombin activity of the most active inhibitors with IC(50)s in the nanomolar range was determined in dogs demonstrating high thrombin inhibitory activity in plasma and an appropriate duration of action after oral administration. (C) 2006 Elsevier Ltd. All rights reserved.
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