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This book investigates and identifies novel therapeutic compounds for the treatment of a range of illnesses. Heterocyclic compounds are a significant class of substances with biological activity. Among them, quinazoline has attracted a lot of interest because of its important biological properties. Numerous compounds with quinazoline moiety have been shown to exhibit a wide range of therapeutic properties, including antioxidant, antifungal, antiviral, antidiabetic, anticancer, anti-inflammatory, and antibacterial activities. This book presents a comprehensive overview of quinazoline and its derivatives. The chapters address recent advances in the synthesis of several different heterocyclic compounds, the use of computational studies for finding new active quinazoline derivatives, the biological activities of quinazoline, and much more.