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ID: ALA1681717
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Authors: Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.
Abstract: 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.
CiteXplore: 21316234