471845-12-2Relevant articles and documents
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold
Graczyk, Piotr P.,Khan, Afzal,Bhatia, Gurpreet S.,Palmer, Vanessa,Medland, Darren,Numata, Hirotoshi,Oinuma, Hitoshi,Catchick, Jacqueline,Dunne, Angela,Ellis, Moira,Smales, Caroline,Whitfield, Jonathan,Neame, Stephen J.,Shah, Bina,Wilton, Daniel,Morgan, Louise,Patel, Toshal,Chung, Raymond,Desmond, Howard,Staddon, James M.,Sato, Nobuaki,Inoue, Atsushi
, p. 4666 - 4670 (2007/10/03)
Imidazole-based structures of p38 inhibitors served as a starting point for the design of JNK3 inhibitors. Construction of a 6,7-dihydro-5H-pyrrolo[1,2-a] imidazole scaffold led to the synthesis of the (S)-enantiomers, which exhibited p38/JNK3 IC50 ratio of up to 10 and were up to 20 times more potent inhibitors of JNK3 than the relevant (R)-enantiomers. The JNK3 inhibitory potency correlated well with inhibition of c-Jun phosphorylation and neuroprotective properties of the compounds in low K+-induced cell death of rat cerebellar granule neurones.