197960-67-1Relevant articles and documents
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
