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  • Title: Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.
    Author: Hanessian S, Simard D, Bayrakdarian M, Therrien E, Nilsson I, Fjellström O.
    Journal: Bioorg Med Chem Lett; 2008 Mar 15; 18(6):1972-6. PubMed ID: 18289852.
    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 P(1) and P(3) sites. Potent in vitro activity against thrombin, with excellent selectivity over trypsin was found for selected analogues.
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