کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1365204 | 981554 | 2008 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Sulfonamidolactam inhibitors of coagulation factor Xa Sulfonamidolactam inhibitors of coagulation factor Xa](/preview/png/1365204.png)
As part of an effort to identify novel backups for previously reported pyrazole-based coagulation Factor Xa inhibitors, the pyrazole 5-carboxamide moiety was replaced by 3-(sulfonylamino)-2-piperidone. This led to the identification of a structurally diverse chemotype that was further optimized to incorporate neutral or weakly basic aryl and heteroaryl P1 groups while maintaining good potency versus Factor Xa. Substitution at the sulfonamide nitrogen provided further improvements in potency and as did introduction of alternate P4 moieties.
The synthesis and SAR of N-aryl-3-(arylsulfonylamino)-piperidone inhibitors of Factor Xa is described. Compound 55 is a representative example of this series with fXa Ki = 0.043 nM.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 7, 1 April 2008, Pages 2428–2433