Title of article
Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs
Author/Authors
Stephen Hanessian، نويسنده , , Daniel Simard، نويسنده , , Malken Bayrakdarian، نويسنده , , Eric Therrien، نويسنده , , Ingemar Nilsson، نويسنده , , Ola Fjellstr?m، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
1972
To page
1976
Abstract
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 P1 and P3 sites. Potent in vitro activity against thrombin, with excellent selectivity over trypsin was found for selected analogues.
Keywords
thrombin , Enzyme inhibitors , 2-pyridone
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799282
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