A Facile Synthesis of New 4,6-Dichloropyridine Derivatives, Their Biological Evaluation for Antimicrobial and Antioxidant Activity, and Docking Studies

作者：Singaram Kulathooran^*; Marimuthu Dhamodaran; Baskaran Selvakumar; Chinaga Sureshkumar

来源：Journal of the Chinese Chemical Society, 2016, 63(9): 758-769.

DOI：10.1002/jccs.201600191

• 4
• 6-Dichloropyridine
• Microwave irradiation
• Antioxidant
• Antimicrobial
• Quantitative structure-activity relationship
• Molecular docking

A facile synthesis of new 4,6-dichloropyridine derivatives 5(a-f), 6(a-c), and 7(a-c) were synthesized using both conventional heating and solvent-free microwave irradiation techniques. The results revealed that the latter method is superior to the conventional heating method. The easy work-up of the products, rapid reaction, and mild conditions are noticeable features of this protocol. Structural elucidation of the synthesized compounds was made on the basis of various spectroscopic methods. The synthesized compounds were evaluated for their in vitro antimicrobial activity (minimum inhibitory concentration; MIC) against various microbial strains using the agar well-diffusion method. Among the compounds, 5c showed best antimicrobial activity against most of the employed strains, especially against Staphylococcus aureus, Escherichia coli, Rhizopus arrhizus, and Candida albicans. Compounds 5a, 6a, 6c, 7a, and 7c showed significant antioxidant activity when compared to the other compounds. In addition to this, theoretical docking studies were performed for the highly potent compounds 5a, 6a, 6c, 7a, and 7c against three different drug targets belonging to the oxidoreductase family, and the results were found to be highly satisfactory.

• 出版日期2016-9