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J Med Chem. 2016 May 26;59(10):4676-87. doi: 10.1021/acs.jmedchem.6b00015. Epub 2016 Apr 22.

Discovery, Optimization, and Biological Evaluation of Sulfonamidoacetamides as an Inducer of Axon Regeneration.

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Bio-Center, Gyeonggi Institute of Science and Technology Promotion , 147 Gwanggyo-ro, Suwon, Korea 16229.
Department of Applied Chemistry, Ajou University , 206 Worldcup-ro, Suwon, Korea 16499.
Department of Pharmacy, Hanyang University , 55 Hanyangdaehak-ro, Ansan, Korea 15588.


Axon regeneration after injury in the central nervous system is hampered in part because if an age-dependent decline in the intrinsic axon growth potential, and one of the strategies to stimulate axon growth in injured neurons involves pharmacological manipulation of implicated signaling pathways. Here we report phenotypic cell-based screen of chemical libraries and structure-activity-guided optimization that resulted in the identification of compound 7p which promotes neurite outgrowth of cultured primary neurons derived from the hippocampus, cerebral cortex, and retina. In an animal model of optic nerve injury, compound 7p was shown to induce growth of GAP-43 positive axons, indicating that the in vitro neurite outgrowth activity of compound 7p translates into stimulation of axon regeneration in vivo. Further optimization of compound 7p and elucidation of the mechanisms by which it elicits axon regeneration in vivo will provide a rational basis for future efforts to enhance treatment strategies.

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