Synthesis, Characterization and Biological Ac...

Synthesis, Characterization and Biological Activity of Aryl Halogenated Heterocyclics, Containing Nitrogen and Sulphur

Author Name : Mr. M. Guruvareddy, Dr. Sunil Gupta, Dr. Abdul Wadood Siddiqui, Mr. Saroj Kumar Yadav

DOI: https://doi.org/10.56025/IJARESM.2024.1211242621

Aryl halogenated heterocycles containing nitrogen and sulfur are crucial scaffolds in medicinal and organic chemistry, exhibiting diverse biological activities and structural adaptability. These compounds demonstrate a range of pharmacological properties, including antimicrobial, anticancer, antiviral, anti-inflammatory, and antioxidant effects. The presence of halogens (fluorine, chlorine, bromine, or iodine) in the aryl ring enhances their biological potency and metabolic stability by modulating electronic properties, hydrophobicity, and target interactions. Nitrogen-containing heterocycles, such as pyridines, pyrimidines, and pyrazoles, act as hydrogen bond donors or acceptors, enabling interactions with enzymes, receptors, and DNA. Sulfur-based groups, including thioethers, thiophenes, and sulfonamides, enhance lipophilicity and provide additional binding sites, further boosting pharmacological activity. The synergy between nitrogen, sulfur, and halogen atoms contributes to improved bioavailability, target specificity, and reduced toxicity. Aryl halogenated heterocycles have shown efficacy against multidrug-resistant pathogens, with halogenated thiazoles and thiophenes disrupting cell wall synthesis or inhibiting essential enzymes. They also exhibit anticancer activity by targeting pathways like PI3K/Akt/mTOR and antiviral effects by blocking viral replication and entry. Synthetic strategies, including halogenation and functional group modifications, are employed to optimize their physicochemical properties and biological activity. Despite their therapeutic potential, challenges such as environmental persistence and off-target effects necessitate green chemistry approaches and structure-activity relationship (SAR) studies. These compounds hold immense promise for developing novel drugs targeting diverse diseases through advanced design and synthesis.