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Potent and efficacious thienylamidine-incorporated thrombin inhibitors
1Biotech Research Institute, LG Chemical Ltd./Research Park, Science Town, Taejon, Korea.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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.