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A highly diastereoselective method for the synthesis of novel <i>spiro</i>-tetrahydroquinoline derivatives is reported here, using a one-pot reaction method. All compounds were characterized by ¹H-nuclear magnetic resonance (NMR) and mass spectroscopy, and their stereo configurations were confirmed by X-ray analysis. These activities of these derivatives were then tested in human keratocyte cells. The responses of cells to treatment with selected compounds were studied using scratch analysis, and the compounds were tested in a mouse excision wound model. Three of the derivatives demonstrated significant wound-healing activities.