187163-88-8Relevant articles and documents
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption
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.
, p. 1719 - 1724 (1998)
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.
