@article{a8768d0591e14df4a2443e47cec34043,
title = "Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines",
abstract = "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.",
author = "Burgey, {Christopher S.} and Robinson, {Kyle A.} and Lyle, {Terry A.} and Sanderson, {Philip E.J.} and Lewis, {S. Dale} and Lucas, {Bobby J.} and Krueger, {Julie A.} and Rominder Singh and Cynthia Miller-Stein and White, {Rebecca B.} and Bradley Wong and Lyle, {Elizabeth A.} and Williams, {Peter D.} and Coburn, {Craig A.} and Dorsey, {Bruce D.} and Barrow, {James C.} and Stranieri, {Maria T.} and Holahan, {Marie A.} and Sitko, {Gary R.} and Cook, {Jacquelynn J.} and McMasters, {Daniel R.} and McDonough, {Colleen M.} and Sanders, {William M.} and Wallace, {Audrey A.} and Clayton, {Franklin C.} and Dennis Bohn and Leonard, {Yvonne M.} and Detwiler, {Theodore J.} and Lynch, {Joseph J.} and Youwei Yan and Zhongguo Chen and Lawrence Kuo and Gardell, {Stephen J.} and Shafer, {Jules A.} and Vacca, {Joseph P.}",
year = "2003",
month = feb,
day = "13",
doi = "10.1021/jm020311f",
language = "English (US)",
volume = "46",
pages = "461--473",
journal = "Journal of medicinal chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "4",
}