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. 2011 Sep 15;21(18):5521-7.
doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7.

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Simeon Bowers  1 , Anh P Truong, R Jeffrey Neitz, Roy K Hom, Jennifer M Sealy, Gary D Probst, David Quincy, Brian Peterson, Wayman Chan, Robert A Galemmo Jr, Andrei W Konradi, Hing L Sham, Gergely Tóth, Hu Pan, May Lin, Nanhua Yao, Dean R Artis, Heather Zhang, Linda Chen, Mark Dryer, Bhushan Samant, Wes Zmolek, Karina Wong, Colin Lorentzen, Erich Goldbach, George Tonn, Kevin P Quinn, John-Michael Sauer, Sarah Wright, Kyle Powell, Lany Ruslim, Zhao Ren, Frédérique Bard, Ted A Yednock, Irene Griswold-Prenner
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Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Simeon Bowers et al. Bioorg Med Chem Lett. .

Abstract

The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification studies which led to compounds such as 42 with lower clearance, greater brain exposure and longer half life compared to earlier analogs.

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