Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement

[Image: see text] Modification of the previously disclosed (S)-N-(2-(aminomethyl)-5-chlorobenzyl)-1-((R)-2-hydroxy-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamide 2 by optimization of the P3 group afforded novel, low molecular weight thrombin inhibitors. Heterocycle replacement of the hydroxyl functi...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Chobanian, Harry R., Pio, Barbara, Guo, Yan, Shen, Hong, Huffman, Mark A., Madeira, Maria, Salituro, Gino, Terebetski, Jenna L., Ormes, James, Jochnowitz, Nina, Hoos, Lizbeth, Zhou, Yuchen, Lewis, Dale, Hawes, Brian, Mitnaul, Lyndon, O’Neill, Kim, Ellsworth, Kenneth, Wang, Liangsu, Biftu, Tesfaye, Duffy, Joseph L.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2015
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4434479/
https://ncbi.nlm.nih.gov/pubmed/26005532
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00047
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