Although the S3 pocket of the thrombin active site is lined with lipophilic amino acid residues, the accommodation of polarity within the lipophilic P3 moiety of small molecule inhibitors is possible provided that the polar functionality is capable of pointing away from the binding pocket outwards t
Metabolism-Directed Optimization of 3-Aminopyrazinone Acetamide Thrombin Inhibitors. Development of an Orally Bioavailable Series Containing P1 and P3 Pyridines
โ Scribed by Burgey, Christopher S.; Robinson, Kyle A.; Lyle, Terry A.; Sanderson, Philip E. J.; Lewis, S. Dale; Lucas, Bobby J.; Krueger, Julie A.; Singh, Rominder; Miller-Stein, Cynthia; White, Rebecca B.; Wong, Bradley; Lyle, Elizabeth A.; Williams, Peter D.; Coburn, Craig A.; Dorsey, Bruce D.; Barrow, James C.; Stranieri, Maria T.; Holahan, Marie A.; Sitko, Gary R.; Cook, Jacquelynn J.; McMasters, Daniel R.; McDonough, Colleen M.; Sanders, William M.; Wallace, Audrey A.; Clayton, Franklin C.; Bohn, Dennis; Leonard, Yvonne M.; Detwiler,, Theodore J.; Lynch,, Joseph J.; Yan, Youwei; Chen, Zhongguo; Kuo, Lawrence; Gardell, Stephen J.; Shafer, Jules A.; Vacca, Joseph P.
- Book ID
- 119957454
- Publisher
- American Chemical Society
- Year
- 2003
- Tongue
- English
- Weight
- 340 KB
- Volume
- 46
- Category
- Article
- ISSN
- 0022-2623
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