Oh Y S, Yun M, Hwang S Y, Hong S, Shin Y, Lee K, Yoon K H, Yoo Y J, Kim D S, Lee S H, Lee Y H, Park H D, Lee C H, Lee S K, Kim S
Biotech Research Institute, LG Chemical LTD, Taejon, Korea.
Bioorg Med Chem Lett. 1998 Mar 17;8(6):631-4. doi: 10.1016/s0960-894x(98)00079-1.
Systematic variation of the so-called P-pocket moiety of benzamidrazone-based selective thrombin inhibitors led to the discovery of LB30057. It is potent (Ki = 0.38 nM for human thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailability in dogs). LB30057 was efficacious in thrombosis animal models.
基于苯甲脒的选择性凝血酶抑制剂所谓P口袋部分的系统变化导致了LB30057的发现。它具有高效性（对人凝血酶的Ki = 0.38 nM）、选择性（对牛胰蛋白酶的Ki = 3290 nM），并且口服生物利用度良好（在犬类中的口服生物利用度为58%）。LB30057在血栓形成动物模型中有效。
