Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
Structure based design techniques were used to exploit the putative similarity in binding mode of an aminopyridinone thrombin inhibitor 2 and a trisubstituted benzene inhibitor 3 to generate a new lead inhibitor 4. Further optimization led to the identification of a novel series of potent thrombin inhibitor 22 with improved physical, chemical stability and in vitro functional potency.
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关键词
Thrombin,Inhibitor,Anticoagulant
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