189339-80-8Relevant academic research and scientific papers
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors
Lu, Tianbao,Tomczuk, Bruce,Illig, Carl R.,Bone, Roger,Murphy, Larry,Spurlino, John,Salemme, F. Raymond,Soll, Richard M.
, p. 1595 - 1600 (2007/10/03)
We describe the in vitro evaluation and crystallographic analysis of a new class of potent and selective, non-aminoacid-based, small-molecule thrombin inhibitors, exemplified by 14. This class of achiral inhibitors lacks an amide-based backbone, exhibits nM inhibition of thrombin, and is selective for thrombin. Compound 14 does not interact with the active-site catalytic apparatus and is anchored to the enzyme via a single network of hydrogen bonds to Asp 189 of the S1 pocket.
GUANIDINO PROTEASE INHIBITORS
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, (2008/06/13)
Compounds of the formula: STR1 wherein R 1--R 4, R. sup.7--R 8, R a, R b, R c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
