1mu6: Difference between revisions

Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2-phenethylamino)-6-methylpyrazinone acetamide template (e.g., 1) which resulted in the modification of each of the three principal components (i.e., P1, P2, P3) comprising this series. As a result of these studies, several potent thrombin inhibitors (e.g., 20, 24, 25) were identified which exhibit high levels of oral bioavailability and long plasma half-lives.

[[Category: Barrow, J C.]]

[[Category: Burgey, C S.]]

[[Category: Clayton, F C.]]

[[Category: Coburn, C A.]]

[[Category: Cook, J J.]]

[[Category: Dorsey, B D.]]

[[Category: Gardell, S J.]]

[[Category: Holahan, M A.]]

[[Category: Jr., J J.Lynch.]]

[[Category: Jr., T J.Detwiler.]]

[[Category: Krueger, J A.]]

[[Category: Leonard, Y M.]]

[[Category: Lewis, S D.]]

[[Category: Lucas, B J.]]

[[Category: Lyle, E A.]]

[[Category: Lyle, T A.]]

[[Category: McDonough, C M.]]

[[Category: McMasters, D R.]]

[[Category: Robinson, K A.]]

[[Category: Sanders, W M.]]

[[Category: Sanderson, P E.]]

[[Category: Shafer, J A.]]

[[Category: Sitko, G R.]]

[[Category: Stranieri, M T.]]

[[Category: Vacca, J P.J.]]

[[Category: Wallace, A A.]]

[[Category: White, R B.]]

[[Category: Williams, P D.]]

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