Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 9, Pages 2865-2870Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.087
Keywords
thrombin inhibitor; trypsin; serine protease; anticoagulant
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2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated in 14, which is a potent thrombin inhibitor (K-i = 1.2 nM) that exhibits robust efficacy in canine anticoagulation and thrombosis models upon oral administration. (c) 2008 Elsevier Ltd. All rights reserved.
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