Enteroviruses (EVs) are common and significant human pathogens in Asia. EV infections can cause a wide spectrum of acute diseases, including CNS complications. These EV infection-related CNS syndromes include acute flaccid paralysis, aseptic meningitis, encephalitis, and even death. Currently, there is no vaccine available for most EVs except for poliovirus; furthermore, there is a lack of clinical antiviral drugs for treating EV-related infections. These shortages reveal the need to develop potent compounds for treating enteroviral infections. This study summarizes the development of drugs for EV-related infections based on molecular targets blocking various steps in the viral replication cycle.