1292805-13-0Relevant articles and documents
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor
Bowers, Simeon,Truong, Anh P.,Neitz, R. Jeffrey,Neitzel, Martin,Probst, Gary D.,Hom, Roy K.,Peterson, Brian,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergley,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Brigham, Elizabeth F.,Quinn, Kevin P.,Sauer, John-Michael,Powell, Kyle,Ruslim, Lany,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
scheme or table, p. 1838 - 1843 (2011/05/05)
The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the 4-position of the thiophene we obtained single digit nanomolar compounds, such as 47, which demonstrated an in vivo effect on JNK activity when dosed orally in our kainic acid mouse model as measured by phospho-c-jun reduction.
