1zgi: Difference between revisions

Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolopyridines. A modification intended to attenuate plasma protein binding (i.e., conversion of the P3 pyridine to a piperidine) conferred significant factor Xa activity to this series. Ultimately, these dual thrombin/factor Xa inhibitors demonstrated excellent in vitro and in vivo anticoagulant efficacy.

[[Category: Burgey, C S.]]

[[Category: Coburn, C A.]]

[[Category: Deng, J Z.]]

[[Category: Krueger, J A.]]

[[Category: Kuo, L C.]]

[[Category: Lewis, S D.]]

[[Category: Lucas, B J.]]

[[Category: Lyle, T A.]]

[[Category: McMasters, D R.]]

[[Category: Rabbat, P M.]]

[[Category: Vacca, J P.]]

[[Category: Williams, P D.]]

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