强效且有效的含噻吩甲脒凝血酶抑制剂。

Potent and efficacious thienylamidine-incorporated thrombin inhibitors.

作者信息

Lee K, Hwang S Y, Yun M, Kim D S

机构信息

Biotech Research Institute, LG Chemical Ltd./Research Park, Science Town, Taejon, Korea.

出版信息

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1683-6. doi: 10.1016/s0960-894x(98)00293-5.

DOI:10.1016/s0960-894x(98)00293-5

Abstract

Novel thrombin inhibitors incorporating thienylamidine at the P1 position were designed and synthesized. These compounds are potent, trypsin-selective and efficacious in the rat model of venous thrombosis. The proposed P1 binding mode in the thrombin active site was confirmed by X-ray crystallographic analysis.

摘要

设计并合成了在P1位含有噻吩基脒的新型凝血酶抑制剂。这些化合物在大鼠静脉血栓形成模型中具有强效、对胰蛋白酶有选择性且有效。凝血酶活性位点中所提出的P1结合模式通过X射线晶体学分析得到了证实。

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