Potent and efficacious thienylamidine-incorporated thrombin inhibitors.
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.
Lee
K
K
Biotech Research Institute, LG Chemical Ltd./Research Park, Science Town, Taejon, Korea.
Hwang
S Y
SY
Yun
M
M
Kim
D S
DS
D000818:Animals; D000991:Antithrombins / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015394:Molecular Structure; D051381:Rats; D013424:Sulfanilamides / Q000737:chemistry*; D013917:Thrombin / Q000737:chemistry
D000991:Antithrombins; D013424:Sulfanilamides; C116659:thienylamidine; D013917:Thrombin