197959-89-0Relevant academic research and scientific papers
AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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Page/Page column 30-31, (2010/11/23)
Amidino and benzamidino compounds, including compounds of the formula: I wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.
Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors
Linusson,Gottfries,Olsson,?rnskov,Folestad,Nordén,Wold
, p. 3424 - 3439 (2007/10/03)
A library of thrombin inhibitors has been designed using statistical molecular design. An aromatic scaffold was used, with three varied positions corresponding to three pockets at the active site of thrombin (the S-, P-, and D-pockets). The selection was
Amidinohydrazones as guanidine bioisosteres: Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors
Soll, Richard M.,Lu, Tianobao,Tomczuk, Bruce,Illig, Carl R.,Fedde, Cynthia,Eisennagel, Stephen,Bone, Roger,Murphy, Larry,Spurlino, John,Salemme, F. Raymond
, p. 1 - 4 (2007/10/03)
We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a non-peptide scaffold. Compound 4 exhibits nM inhibition of thrombin, is selective for thrombin, and
Structure-activity and crystallographic analysis of a new class of non- amide-based thrombin inhibitor
Lu, Tianbao,Soll, Richard M.,Illig, Carl R.,Bone, Roger,Murphy, Larry,Spurlino, John,Salemme, F. Raymond,Tomczuk, Bruce E.
, p. 79 - 82 (2007/10/03)
The structure-activity relationships of a novel series of non-amide- based thrombin inhibitors are described. Exploration of the P2 and the aryl binding region for this series has identified optimal groups for achieving nanomolar potency. The binding modes of these optimal groups have been confirmed by X-ray structural analysis.
AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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, (2008/06/13)
Amidino and benzamidino compounds, including compounds of the formula: STR1 wherein R 1-R 4, R 6-R 9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.
