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Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.

Description : The synthesis of novel coumarins bearing on the lateral side chain in the 3-position an amine or a guanidine group is described. In vitro evaluation highlighted 14d which possesses a meta aniline side chain as a very potent THR inhibitor. Surprisingly, the introduction of a guanidine moiety always l...
Language(s) : English
Subject(s) : Antithrombins , Binding Sites , Coumarins , Models, Molecular , Water
Publisher(s) :
Contributor(s) : FUNDP
Source(s) :
Publication Date(s) : 2006-01-01