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The broad range of medicinal applications of quinazolinone scaffolds has drawn much interest in biological sciences. Almost 200 different organic alkaloids have a family of fused heterocycles that make up their analogues in heterocyclic chemistry. Quinazolines and quinazolinones are a specialized type of heterocyclic compounds having a benzene ring and pyrimidine ring, and due to their manifold uses, heterocyclic scaffolds are well-known for their versatility. The biological prospects of quinazolinone derivatives and their therapeutic applications, such as antimicrobial, anticancer, analgesic, antihypertensive, antiviral, antimalarial, antibacterial, and antifungal activities, are significant for treating the diseases. A number of quinazolinone derivatives have been reviewed here, emphasizing their notable biological and therapeutic applications upon their interactions with enzymes and receptors. The quinazolinone-bearing molecules have shown a number of therapeutic applications, which have been compiled in this updated review.
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