Isaacs R C, Cutrona K J, Newton C L, Sanderson P E, Solinsky M G, Baskin E P, Chen I W, Cooper C M, Cook J J, Gardell S J, Lewis S D, Lucas R J, Lyle E A, Lynch J J, Naylor-Olsen A M, Stranieri M T, Vastag K, Vacca J P
Department of Biological Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 1998 Jul 7;8(13):1719-24. doi: 10.1016/s0960-894x(98)00297-2.
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 methyl 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.
1（L-374,087）是一种强效、选择性、有效且口服生物可利用的凝血酶抑制剂，其含有核心3-氨基-2-吡啶酮部分。将1的C6吡啶酮甲基用丙基取代得到5（L-375,052），它保留了1的所有优异特性，并且在犬和大鼠口服给药后还产生了更高的血浆水平。
