The article discusses the medicinal chemistry of drugs containing N-oxide functionalities, emphasizing their significance in biomedical applications. N-oxides are versatile compounds found in nature and used in drug development, surface engineering, and as prodrugs or polymers. They offer properties such as water solubility, reduced membrane permeability, and redox reactivity, which are crucial for drug targeting and cytotoxicity. The article highlights the synthesis of N-oxides, their chemical and physical properties, and their applications in medicinal chemistry. It also explores their role in natural products, drug development, and polymer-based materials. N-oxides are noted for their stealth properties, making them suitable for drug conjugation and surface engineering. The article covers their use in hypoxia-activated prodrugs, contrast agents for MRI, and antimicrobial applications. It also discusses the challenges and future directions in utilizing N-oxides in healthcare, including their potential in targeted therapies and biocompatible materials. Overall, the article provides a comprehensive overview of the importance and diverse applications of N-oxides in modern medicine.The article discusses the medicinal chemistry of drugs containing N-oxide functionalities, emphasizing their significance in biomedical applications. N-oxides are versatile compounds found in nature and used in drug development, surface engineering, and as prodrugs or polymers. They offer properties such as water solubility, reduced membrane permeability, and redox reactivity, which are crucial for drug targeting and cytotoxicity. The article highlights the synthesis of N-oxides, their chemical and physical properties, and their applications in medicinal chemistry. It also explores their role in natural products, drug development, and polymer-based materials. N-oxides are noted for their stealth properties, making them suitable for drug conjugation and surface engineering. The article covers their use in hypoxia-activated prodrugs, contrast agents for MRI, and antimicrobial applications. It also discusses the challenges and future directions in utilizing N-oxides in healthcare, including their potential in targeted therapies and biocompatible materials. Overall, the article provides a comprehensive overview of the importance and diverse applications of N-oxides in modern medicine.