187163-71-9Relevant articles and documents
P2 pyridine N-oxide thrombin inhibitors: A novel peptidomimetic scaffold
Nantermet, Philippe G.,Burgey, Christopher S.,Robinson, Kyle A.,Pellicore, Janetta M.,Newton, Christina L.,Deng, James Z.,Selnick, Harold G.,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,Miller-Stein, Cynthia,White, Rebecca B.,Wong, Bradley,McMasters, Daniel R.,Wallace, Audrey A.,Lynch Jr., Joseph J.,Yan, Youwei,Chen, Zhongguo,Kuo, Lawrence,Gardell, Stephen J.,Shafer, Jules A.,Vacca, Joseph P.,Lyle, Terry A.
, p. 2771 - 2775 (2007/10/03)
In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxidative metabolism, it also overcomes the metabolic liability associated with the pyrazinones. An optimization study of the P 1 benzylamide delivered the potent thrombin inhibitor 21 (K i = 3.2 nM, 2xaPTT = 360 nM), which exhibited good plasma levels and half-life after oral dosing in the dog (Cmax = 2.6 μM, t 1/2 = 4.5 h).
PYRAZINONE THROMBIN INHIBITORS
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, (2008/06/13)
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PYRIDINONE THROMBIN INHIBITORS
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: STR1 for example: STR2
