439117-43-8Relevant articles and documents
Improved stability of proline-derived direct thrombin inhibitors through hydroxyl to heterocycle replacement
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.
, p. 553 - 557 (2015)
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 replace
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability
Morrissette, Matthew M.,Stauffer, Kenneth J.,Williams, Peter D.,Lyle, Terry A.,Vacca, Joseph P.,Krueger, Julie A.,Lewis, S. Dale,Lucas, Bobby J.,Wong, Bradley K.,White, Rebecca B.,Miller-Stein, Cynthia,Lyle, Elizabeth A.,Wallace, Audrey A.,Leonard, Yvonne M.,Welsh, Denise C.,Lynch, Joseph J.,McMasters, Daniel R.
, p. 4161 - 4164 (2007/10/03)
Modification of lead compound 1 by reducing lipophilicity in the P3 group produced a series of low molecular weight thrombin inhibitors with excellent potency in functional assays, metabolic stability, and oral bioavailability. These modifications led to
