review · Archiv der Pharmazie
Quinazoline and quinazolinone derivatives represent significant chemical scaffolds in medicinal chemistry for creating novel therapeutic candidates. These compounds serve as vital starting points for synthesising a wide range of biologically meaningful and pharmacologically active molecules. Research into their properties reveals broad therapeutic potential, including anticancer, anti-inflammatory, antidiabetic, anticonvulsant, antiviral, and antimicrobial activities. Emerging insights into how these derivatives interact with biological systems create valuable openings for designing new medical treatments. Recent advances cover novel chemical synthetic strategies alongside key medicinal chemistry elements such as rational drug design, structure-activity relationship profiling, and the specific mechanisms of action through which the molecules exert their effects. Bringing together these synthetic approaches and biological mechanisms aims to support the ongoing discovery and targeted development of effective quinazoline and quinazolinone drug candidates.
Quinazoline and quinazolinone molecules offer diverse biological activities that address several major health challenges, including infectious diseases, diabetes, and cancer. A deeper understanding of their chemical synthesis and biological behaviour helps pharmaceutical researchers design more targeted, effective medicines. Consolidating synthetic routes and mechanisms of action accelerates the discovery of potential therapies for conditions that currently lack sufficient treatments.
This review supports early-stage discovery for pharmaceutical companies and medicinal chemists seeking to design novel therapeutics across oncology, infectious diseases, and metabolic conditions. Because the focus is on chemical synthesis methods, structure-activity relationships, and biological mechanisms, the work sits at an early, pre-clinical stage of the drug development pipeline. Practical commercialisation will require further laboratory synthesis, safety profiling, and biological validation before viable drug candidates can advance toward clinical trials.
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Quinazoline and quinazolinone derivatives piqued medicinal chemistry interest in developing novel drug candidates owing to their pharmacological potential. They are important chemicals for the synthesis of a variety of physiologically significant and pharmacologically useful molecules. Quinazoline and quinazolinone derivatives have anticancer, anti-inflammatory, antidiabetic, anticonvulsant, antiviral, and antimicrobial potential. The increased understanding of quinazoline and quinazolinone derivatives in biological activities provides opportunities for new medicinal products. The present review focuses on novel advances in the synthesis of these important scaffolds and other medicinal aspects involving drug design, structure-activity relationship, and action mechanisms of quinazoline and quinazolinone derivatives to help in the development of new quinazoline and quinazolinone derivatives.
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DOI: 10.1002/ardp.202400057
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