Bioorganic and Medicinal Chemistry Letters p. 1719 - 1724 (1998)
Update date:2022-08-03
Topics:
Isaacs, Richard C. A.
Cutrona, Kellie J.
Newton, Christina L.
Sanderson, Philip E. J.
Solinsky, Mark G.
Baskin, Elizabeth P.
Chen, I-Wu
Cooper, Carolyn M.
Cook, Jacquelynn J.
Gardell, Stephen J.
Lewis, S. Dale
Lucas Jr., Robert J.
Lyle, Elizabeth A.
Lynch Jr., Joseph J.
Naylor-Olsen, Adel M.
Stranieri, Maria T.
Vastag, Kari
Vacca, Joseph P.
1 (L-374,087) is a potent, selective, efficacious, and orally bioavailable thrombin inhibitor that contains a core 3-amino-2-pyridinone moiety. Replacement of the C6 pyridinone metyl group of 1 by a propyl group gave 5 (L-375,052), which retained all the excellent properties of 1, and also yielded higher plasma levels after oral dosing in dogs and rats.
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