Evidence map›Paper›PMID 41147282›Full record

ArticleCurrent pharmaceutical design2026

Design and Synthesis of Novel Spiropyridine Derivatives as Promising Anti-inflammatory and Gene-targeting Agents Against COVID-19.

Rita M Borik, Mohammed A Hussein, Hanan A A Farrag, Enas A Taha

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Article in Current pharmaceutical design, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 · Who and what money

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4 authors.

Rita M BorikDepartment of Physical Sciences, Chemistry Division, College of Science, Jazan University, P.O. Box. 114, Jazan, 45142, Saudia Arabia.
Mohammed A HusseinBiotechnology Department, Faculty of Applied Health Science Technology, October 6 University, Giza, 28125, Egypt.ORCID 0000-0002-1811-2794
Hanan A A FarragOrganic Chemistry, Sattam Bin Abdulaziz University, Al Kharj Basic Sciences - First Common Year, KSA, Al Kharj, Saudia Arabia.
Enas A TahaChemistry Department, Faculty of Pharmacy, October 6 University, 6 October City, Giza, 12585, Egypt.ORCID 0000-0003-4786-8037

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundThe COVID-19 pandemic, caused by SARS-CoV-2, has highlighted the urgent need for effective antiviral and anti-inflammatory therapies. Spiropyridine derivatives containing a chalcone moiety have shown potential in targeting key enzymes involved in viral replication and inflammation.

objectiveTo evaluate the inhibitory effects of synthesized spiropyridine derivatives on SARS-CoV-2 main protease (Mpro), secreted phospholipase A2 (sPLA2), and cytosolic phospholipase A2 (cPLA2), and to assess their impact on inflammatory and oxidative stress markers in LPS-treated lung cells.

aimTo develop novel therapeutic agents that can effectively manage COVID-19 and related inflammatory conditions.

methodsThe synthesized compounds (1-3) were tested for their inhibitory activity against SARS-CoV-2 Mpro, sPLA2, and cPLA2 using in vitro assays to determine IC50 values. Inflammatory markers (COX-2, IL-2, IL-4, TGF-1β, TNF-α) and oxidative stress markers (GSH, SOD, GR, MDA) were measured in LPS-treated lung cells. Gene expression levels of sPLA2 and cPLA2 were also assessed. Molecular docking studies were conducted to analyze the binding affinities and interactions of the compounds with the target enzymes.

resultsCompounds 1-3 showed significant inhibitory activity against SARS-CoV-2 Mpro with IC DISCUSSION: The results demonstrate that the structural integration of a spiropyridine core with a chalcone moiety yields compounds with superior multi-target inhibitory activity. The potent antiviral, anti-inflammatory, and antioxidant effects are significantly correlated with their strong binding interactions with the active sites of Mpro, sPLA2, and cPLA2, as validated by molecular docking. These findings align with and extend current research on targeting host-inflammatory pathways alongside viral replication for COVID-19 management.

conclusionThe synthesized spiropyridine derivatives containing a chalcone moiety exhibit potent antiviral, antiinflammatory, and antioxidant properties. These findings suggest that these compounds could be promising therapeutic agents for managing COVID-19 and related inflammatory conditions. Future studies should focus on in vivo experiments, clinical trials, and structural optimization to further develop these compounds for clinical use.

Indexed as

Anti-Inflammatory AgentsAntiviral AgentsCOVID-19 Drug TreatmentDrug DesignPyridinesSARS-CoV-2Coronavirus 3C ProteasesCOVID-19HumansLipopolysaccharidesMolecular Docking SimulationOxidative StressPhospholipases A2, SecretoryAnti-Inflammatory AgentsAntiviral AgentsCoronavirus 3C ProteasesLipopolysaccharidesPhospholipases A2, SecretoryPyridinesanti-inflammatoryantioxidantchalcone moietyCOVID-19molecular dockingphospholipase A2SARS-CoV-2 main proteaseSpiropyridine derivatives

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PMID41147282

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