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Design and Synthesis of a Series of Potent and Orally Bioavailable Noncovalent Thrombin Inhibitors That Utilize Nonbasic Groups in the P1 Position

โœ Scribed by Tucker, Thomas J.; Brady, Stephen F.; Lumma, William C.; Lewis, S. Dale; Gardell, Stephen J.; Naylor-Olsen, Adel M.; Yan, Youwei; Sisko, Jack T.; Stauffer, Kenneth J.; Lucas, Bobby J.


Book ID
115528146
Publisher
American Chemical Society
Year
1998
Tongue
English
Weight
251 KB
Volume
41
Category
Article
ISSN
0022-2623

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โœ Richard C.A. Isaacs; Christina L. Newton; Kellie J. Cutrona; Swati P. Mercer; Br ๐Ÿ“‚ Article ๐Ÿ“… 2011 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 524 KB

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