Title : Quinazolines: Green synthesis, characterization and biological activities
Abstract:
This research explores the synthesis, characterization, and biological evaluation of quinazoline derivatives using green chemistry principles for sustainable pharmaceutical development. By adopting environmentally responsible strategies—such as using renewable feedstocks, non-toxic solvents, and energy-efficient techniques—the study aims to reduce the ecological footprint associated with conventional organic synthesis. These methods not only lower hazardous waste and energy usage but also enhance cost-effectiveness and environmental safety. The synthesized quinazolines are evaluated for their antibacterial, antifungal, and antiviral properties, emphasizing their potential as sustainable alternatives in modern drug development. This research highlights the integration of green chemistry into heterocyclic drug synthesis. Nitrogen-containing heterocycles are indispensable in medicinal chemistry due to their vast biological and therapeutic potential. These structures appear in over 90% of newly approved drugs and play vital roles in pharmaceuticals, agrochemicals, and veterinary medicine. Alkaloidal nitrogen compounds, in particular, significantly influence metabolic pathways and therapeutic activities. Quinazoline, a notable heterocycle first synthesized in 1869, serves as a privileged scaffold in drug design. It is associated with a wide spectrum of biological activities, including antibacterial, anticancer, antihypertensive, anti-inflammatory, and antimalarial properties. Notable derivatives like Gefitinib and Erlotinib are used effectively in cancer therapy. Recent advances in synthetic methodologies—such as phase-transfer catalysis, microwave-assisted synthesis, and metal-catalyzed reactions—have greatly expanded the biological applications of quinazolines. In parallel, thiophenes and benzothiophenes, synthesized via Grignard reactions, cyclization, and Suzuki coupling, exhibit potent antibacterial and anticancer properties. Pyrazoles, synthesized through hydrazine condensation and ring closure, are also known for their antimicrobial, antifungal, and anticancer activities. The alarming rise of multidrug-resistant bacteria calls for novel antibacterial agents. Our research investigates the synthesis of quinazolin-2-amines coupled with thiophene or pyrazole moieties. While these pharmacophores have been explored individually, their combination is a novel strategy that could enhance antibacterial efficacy and open new directions in drug discovery.
