کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373183 | 981891 | 2011 | 5 صفحه PDF | دانلود رایگان |

A novel 1,3,5-trisubstituted benzamide thrombin inhibitor template was designed via hybridization of a known aminopyridinoneacetamide and a known 1,3,5-trisubstituted phenyl ether. Optimization of this lead afforded a novel potent series of biaryl 1,3,5-trisubstituted benzenes with excellent functional anticoagulant potency.
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.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1536–1540