Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 6, Pages 1972-1976Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.122
Keywords
enzyme inhibitors; thrombin; 2-pyridone
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Guided by available X-ray crystal structure data on the serine protease thrombin, a series of pyridin-2-one derivatives were designed and synthesized having diverse functionality at the P-1 and P-3 sites. Potent in vitro activity against thrombin, with excellent selectivity over trypsin was found for selected analogues. (C) 2008 Elsevier Ltd. All rights reserved.
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