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An Improved Regiospecific Synthesis of [1,2,4]-Thiadiazolo[4,3-a]pyridine Imines in Green Media and Its Significance in Biological Systems
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DOI：10.1002/ajoc.70468.png)
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Abstract
En 中文
Numerous drugs with important pharmaceutical roles are known to possess heterocyclics as key scaffolds. In this study, a series of novel [1,2,4]-thiadiazolo[4,3-a]pyridine imine derivatives were designed and synthesized following microwave assisted green synthetic approach and further characterized employing various analytical methods. This regiospecific approach involves the activation of isothiocyanate moiety by I2 followed by nucleophillic attack and base catalyzed intramolecular cyclization to generate the title compounds under green microwave conditions. The synthetic methodology addresses the limitations of conventional methods by utilizing commercially available chemicals in green media, eliminating the need for hazardous solvents, expensive metal catalysts, or specialized electrochemical equipment. The biological importance of these compounds was also assessed by their ability to bind with biomolecules like proteins and nucleic acids. It was revealed that the derivatives with longer alkyl chain showed excellent binding to proteins via hydrophobic interactions while derivatives with aromatic substituents revealed stronger binding with nucleic acids due to pi-stacking interactions. Further, anti-oxidant potentials of all the derivatives as evaluated through DPPH and hydroxyl radical scavenging assays along with reducing power evaluations have revealed that derivatives with electron donating substituents showed good antioxidant potentials. The anti-bacterial properties of these derivatives were also investigated against gram-positive and gram-negative bacteria.
Keywords:
antibacterials
antioxidants
green synthesis
heterocycles
molecular docking
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