Natural Product‐Derived Semisynthetic Drugs for Neurological Disorders

ABSTRACT Neurological disorders, including neurodegenerative diseases, epilepsy, and psychiatric conditions, pose significant global health challenges, necessitating the continuous search for effective therapeutic agents. Natural products have long served as potential source of bioactive compounds, many of which have been successfully developed into FDA‐approved drugs for neurological disorders. Since the discovery of morphine two centuries ago, natural products have continued to serve as the predominant source of novel drugs and scaffolds for treating CNS disorders. This review provides a focused, case‐study based review of selected semisynthetic neurological drugs, critically examining the semisynthetic optimization and clinical translation of natural product‐derived neurological drugs. By highlighting how targeted chemical modifications have converted complex or suboptimal natural products into successful CNS drugs, the review illustrates both the opportunities and challenges in advancing natural products toward regulatory approval. This review underscores the continuing potential of natural products in drug discovery and inspires future research into novel neurotherapeutics.