article · ChemMedChem
Limited therapeutic treatments exist for SARS-CoV-2, motivating the creation of new antiviral candidates. A series of pyrazine-based small molecules was produced using microwave-assisted click chemistry and benzotriazole chemistry methods. Following laboratory synthesis, all resulting conjugates were tested directly against the SARS-CoV-2 virus to measure their antiviral effectiveness and evaluate cellular toxicity. Computational modelling was also performed to confirm and support the laboratory findings. Across the tested compounds, specific pyrazine-triazole conjugates alongside a particular pyrazine-carboxamide conjugate demonstrated marked antiviral potency against the virus. Furthermore, evaluations of their selectivity indices revealed that these top-performing compounds exhibited meaningful efficacy when compared directly against the established reference drug, Favipiravir.
The ongoing need for effective antiviral treatments against SARS-CoV-2 demands new chemical candidates that can stop viral activity without causing harm to host cells. Demonstrating that novel pyrazine conjugates can outperform standard reference drugs such as Favipiravir in early laboratory efficacy tests helps identify viable starting points for developing targeted coronavirus therapies.
This early-stage research provides potential lead compounds for pharmaceutical developers and medicinal chemists working on SARS-CoV-2 therapeutics. Because testing has only progressed through chemical synthesis, computer modelling, and initial laboratory screening, these molecules remain at an early discovery stage. Significant further preclinical optimisation, toxicity testing, and animal trials will be required before any clinical or commercial application can be pursued.
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Currently, limited therapeutic options are available for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). We have developed a set of pyrazine-based small molecules. A series of pyrazine conjugates was synthesized by microwave-assisted click chemistry and benzotriazole chemistry. All the synthesized conjugates were screened against the SAR-CoV-2 virus and their cytotoxicity was determined. Computational studies were carried out to validate the biological data. Some of the pyrazine-triazole conjugates (5 d-g) and (S)-N-(1-(benzo[d]thiazol-2-yl)-2-phenylethyl)pyrazine-2-carboxamide 12 i show significant potency against SARS-CoV-2 among the synthesized conjugates. The selectivity index (SI) of potent conjugates indicates significant efficacy compared to the reference drug (Favipiravir).
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DOI: 10.1002/cmdc.202100476
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