TY - JOUR AU - 남태규 DA - 2016/05 PY - 2016 UR - https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b00015 UR - https://repository.hanyang.ac.kr/handle/20.500.11754/102306 AB - 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. PB - AMER CHEMICAL SOC KW - SPINAL-CORD-INJURY KW - NEURONS KW - CELLS KW - INHIBITION KW - EXPRESSION KW - FAMILY KW - RAT KW - CNS TI - Discovery, Optimization, and Biological Evaluation of Sulfonamidoacetamides as an Inducer of Axon Regeneration IS - 10 VL - 59 DO - 10.1021/acs.jmedchem.6b00015 T2 - JOURNAL OF MEDICINAL CHEMISTRY ER -