Synthesis and Biological Activity of Novel 5-(ω-Aryloxyalkyl)oxazole Derivatives as Brain-Derived Neurotrophic Factor Inducers

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A novel series of 5-(ω-aryloxyalkyl)oxazole derivatives was prepared and their effects on brain-derived neurotrophic factor (BDNF) production were evaluated in human neuroblastema (SK-N-SH) cells. Syntheses were performed by construction of an oxazole ring as a key reaction. Most of the 5-(ω-aryloxyalkyl)oxazole derivatives markedly increased BDNF production in SK-N-SH cells. 4-(4-Chlorophenyl)-2-(2-methyl-1H-imidazol-l-yl)-5-[3-(2-methoxyphenoxy)propyl]-l,3-oxazole, one of the most promising compounds, showed potent activity (EC_<50>=7.9μM) and the improvement of the motor nerve conduction velocity and the tail-flick response accompanied by a recovery of the brain-derived neurotrophic factor level in the sciatic nerve of streptozotocin (STZ)-diabetic rats.
公益社団法人日本薬学会の論文
2003-05-01