Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: The advances continue

• Quinazolines and quinazolinones are promising bioactive scaffolds in medicinal chemistry.
• Mild, efficient and environmentally benign procedures employed for synthesis are focused.
• Proposed mechanistic investigations have also been concentrated.
• Useful synthetic applications and product manipulations have been displayed.
• A diverse spectrum of biological activities has been presented.

The presence of N-heterocycles as an essential structural motif in a variety of biologically active substances has stimulated the development of new strategies and technologies for their synthesis. Among the various N-heterocyclic scaffolds, quinazolines and quinazolinones form a privileged class of compounds with their diverse spectrum of therapeutic potential. The easy generation of complex molecular diversity through broadly applicable, cost-effective, practical and sustainable synthetic methods in a straightforward fashion along with the importance of these motifs in medicinal chemistry, received significant attention from researchers engaged in drug design and heterocyclic methodology development. In this perspective, the current review article is an effort to recapitulate recent developments in the eco-friendly and green procedures for the construction of highly challenging and potentially bioactive quinazoline and quinazolinone compounds in order to help medicinal chemists in designing and synthesizing novel and potent compounds for the treatment of different disorders. The key mechanistic insights for the synthesis of these heterocycles along with potential applications and manipulations of the products have also been conferred. This article also aims to highlight the promising future directions for the easy access to these frameworks in addition to the identification of more potent and specific products for numerous biological targets.

The current review article summarizes the recent developments in synthetic methodologies for the construction of quinazoline and quinazolinone heterocycles. Mechanistic investigations, applications, product manipulations and biological potential have also been discussed.Figure optionsDownload as PowerPoint slide