Exploring Novel Ester Linked 1,4-Disubstituted 1, 2, 3 Triazole Derivatives: Design, Regioselective Synthesis and Antiviral Activity as Hemagglutinin and Neuraminidase Inhibitors

1, 2, 3 triazoles and its derivatives plays crucial role in medicinal chemistry. They emerged as a pharmacologically significant scaffold in several viral infections due to its broad spectrum and potent activity. Severe viral Diseases like Covid-19, Ebola virus, Swine Flu are emerging now a day and are found fatal. Currently a very few of antiviral chemotherapeutic agents available, It is essential to prioritize the development of potential antiviral drugs to combat the spread of deadly viral infections. The current study involves the combination of Alkyne and Azide through the convenient Copper catalysed 1,3-dipolar cycloaddition of Huisgen’s reaction approach to form 1, 4-disubstituted (regioselective) ester linked 1,2,3-triazoles. The reaction was mediated by Sodium Ascorbate, whereas Cu(I) was used as an efficient, non-toxic and easily available inorganic catalyst. Newly prepared derivatives are identified and assured by thin layer Chromatography, Physical constant and other spectroscopic methods like Infrared, NMR 1H and 13C and Mass. Raised atom economy, good yields, mild reaction condition and low environmental impact makes this process is of considerable synthetic advantages. Assessment of the synthesized compounds for antiviral activity demonstrated their optimum effectiveness against the (H1N1) influenza Swine Flu virus.

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Publication Details

Journal
International Journal of Pharmaceutical Quality Assurance
Published
2024-12-25
DOI
https://doi.org/10.25258/ijpqa.15.4.33
Primary Topic
Synthesis and Characterization of Heterocyclic Compounds
Type
article
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article

Exploring Novel Ester Linked 1,4-Disubstituted 1, 2, 3 Triazole Derivatives: Design, Regioselective Synthesis and Antiviral Activity as Hemagglutinin and Neuraminidase Inhibitors

Chopade Pavankumar D, Shaikh Anwar Rafique
International Journal of Pharmaceutical Quality Assurance
Synthesis and Characterization of Heterocyclic Compounds
article

Exploring Novel Ester Linked 1,4-Disubstituted 1, 2, 3 Triazole Derivatives: Design, Regioselective Synthesis and Antiviral Activity as Hemagglutinin and Neuraminidase Inhibitors

Chopade Pavankumar D, Shaikh Anwar Rafique
article en

Abstract

1, 2, 3 triazoles and its derivatives plays crucial role in medicinal chemistry. They emerged as a pharmacologically significant scaffold in several viral infections due to its broad spectrum and potent activity. Severe viral Diseases like Covid-19, Ebola virus, Swine Flu are emerging now a day and are found fatal. Currently a very few of antiviral chemotherapeutic agents available, It is essential to prioritize the development of potential antiviral drugs to combat the spread of deadly viral infections. The current study involves the combination of Alkyne and Azide through the convenient Copper catalysed 1,3-dipolar cycloaddition of Huisgen’s reaction approach to form 1, 4-disubstituted (regioselective) ester linked 1,2,3-triazoles. The reaction was mediated by Sodium Ascorbate, whereas Cu(I) was used as an efficient, non-toxic and easily available inorganic catalyst. Newly prepared derivatives are identified and assured by thin layer Chromatography, Physical constant and other spectroscopic methods like Infrared, NMR 1H and 13C and Mass. Raised atom economy, good yields, mild reaction condition and low environmental impact makes this process is of considerable synthetic advantages. Assessment of the synthesized compounds for antiviral activity demonstrated their optimum effectiveness against the (H1N1) influenza Swine Flu virus.

International Journal of Pharmaceutical Quality Assurance
Openalex Percentile: Top 80%
Synthesis and Characterization of Heterocyclic Compounds
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