Natural products have long served as a rich source of lead compounds for drug discovery and development. However, their inherent limitations, such as poor bioavailability, selectivity and metabolic instability, often hinder their clinical utility. Medicinal chemistry strategies play a pivotal role in overcoming these challenges by modifying bioactive natural products to enhance their pharmacological properties. This article provides an overview of various medicinal chemistry approaches employed for the modification of bioactive natural products, including structural optimization, semi-synthesis, prodrug design and molecular hybridization. Case studies highlighting successful examples of these strategies in drug development are also discussed.
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