Stroke is a central nervous system disease that seriously affects people's quality of life and has the second highest rate of morbidity and mortality in the world. At present, clinical treatment strategies for acute ischemic stroke are mainly thrombolytic and thrombectomy therapy. However, these strategies are not able to protect patients from ischemic injuries. Therefore, treatment should further focus on methods that improve the survival rate of neurons around the ischemic area and neurological function. This article reviews current research and developments regarding small molecular compounds, including natural products and newly synthesized compounds that have neuroprotective effects and potential molecular targets for the recovery of post-ischemic stroke neural function that have been identified through lab investigations conducted during the last five years. Although pre-clinical studies of these compounds may not be immediately successful, current findings suggest that these therapeutic targets and neuroprotective agents are promising.