862205-50-3Relevant academic research and scientific papers
Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs
Hanessian, Stephen,Simard, Daniel,Bayrakdarian, Malken,Therrien, Eric,Nilsson, Ingemar,Fjellstroem, Ola
, p. 1972 - 1976 (2008/12/22)
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 again
NEW PYRIDIN-2-ONE COMPOUNDS USEFUL AS INHIBITORS OF THROMBIN
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Page/Page column 104-105, (2008/06/13)
There is provided a compound of formula I, wherein the dashed line, R1, R2, R3a, R3b, A, D, E, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).
