197959-99-2Relevant academic research and scientific papers
AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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Page/Page column 33, (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.
Oxyguanidines: Application to non-peptidic phenyl-based thrombin inhibitors
Tomczuk, Bruce,Lu, Tianbao,Soll, Richard M.,Fedde, Cynthia,Wang, Aihua,Murphy, Larry,Crysler, Carl,Dasgupta, Malini,Eisennagel, Stephen,Spurlino, John,Bone, Roger
, p. 1495 - 1498 (2007/10/03)
Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics.
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
