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Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors. |
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| Authors: | M R Becker W R Ewing R S Davis H W Pauls C Ly A Li H J Mason Y M Choi-Sledeski A P Spada V Chu K D Brown D J Colussi R J Leadley R Bentley J Bostwick C Kasiewski S Morgan |
| Affiliation: | 1. Department of Chemistry, Faculty of Sciences, Shahid Chamran University of Ahvaz, Ahvaz, Iran;2. Department of Chemistry, La Trobe University, Bundoora Victoria 3086, Australia;1. Department of Pathology, the First Bethune Hospital of Jilin University, Changchun, Jilin 130021, China;2. Sichuan Academy of Medical Sciences & Sichuan Provincial People''s Hospital, Chengdu, Sichuan 610000, China;3. Department of Gastrointestinal Colorectal and Surgery, China-Japan Union Hospital of Jilin University, Changchun, Jilin 130031, China |
| Abstract: | Thienopyridine sulfonamide pyrrolidinones were found to be potent and selective inhibitors of the coagulation cascade enzyme factor Xa. SAR studies led to several compounds that were selected for further in vivo investigation. These novel aryl binding pocket moieties represent a structural modification to a series of fXa inhibitors. Several compounds proved to be efficacious i.v. antithrombotic agents. |
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