Quinazolinone as Bioactive Pharmacophore: Synthesis and Biological Activities

Quinazolinone, a nitrogen-containing bicyclic system having a benzene-fused pyrimidine ring, constitutes an important organic framework that has attracted the interest of all scientists working in the pharmacological and agricultural sectors owing to its numerous biological properties. Synthetic accessibility and structural flexibility allowed this skeleton to be easily modified with certain reagents that enhance its physicochemical properties. The aim of this review is to study the structural modifications of quinazolinone by various methods, suited for controlling virulence caused by various pathogens. Synthesis of quinazolinone derivatives and their potential hybrid skeletons with different heterocyclic moieties has also been explored. Furthermore, covering its applications from the well-established field of drug discovery to its innovative potential in crop protection, cancer treatment, microbial infections, insomnia, viral diseases, and so forth, has been reviewed with a concise discussion of their structure-activity relationships (SAR). In addition, it was deduced that modifying quinazolinone with electron-donating and electron-withdrawing substituents and heterocyclic moieties had escalated their biological aptitude in comparison to the basic quinazolinone moiety. This study can direct researchers working in this field to adopt a new approach for formulating and optimizing the synthesis and therapeutic potential of quinazolinone derivatives.