Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
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Page column 48
(2010/02/06)
D-Phe-Pro-Arg type thrombin inhibitors: Unexpected selectivity by modification of the P1 moiety
Synthesis of thrombin inhibitors and their binding mode to thrombin is described. Modification of the P1 moiety leads to an increased selectivity versus trypsin. The observed selectivity is discussed in view of their thrombin-inhibitor complex X-ray struc
Lange, Udo E. W.,Baucke, Dorit,Hornberger, Wilfried,Mack, Helmut,Seitz, Werner,Hoeffken, H. Wolfgang
p. 2029 - 2033
(2007/10/03)
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