K36-based inhibitor analogs as potential therapeutics against SARS-CoV-2 main protease (Mpro): a computational investigation.

Publication date: Jun 23, 2025

The global pandemic caused by SARS-CoV-2 has underscored the critical necessity for effective antiviral therapies. The viral main protease (Mpro), crucial for viral replication, has emerged as a promising therapeutic target. In the present study, the inhibitory potential of ten drug-like compounds (KL1-KL10), designed as derivatives of the parent inhibitor K36, against Mpro, has been computationally investigated. To elucidate the binding affinities and interactions of the suggested drugs with the Mpro active site, molecular docking and molecular dynamics (MD) simulations till 500 nanoseconds have been applied. Our results revealed that many suggested inhibitors exhibited enhanced binding affinities compared to the parent inhibitor K36. Among these, KL7 displayed the most favourable binding characteristics, with a docking score of -13. 54 and MM-PBSA binding energy of -34. 57 kJ/mol, surpassing that of K36. Molecular dynamics simulations demonstrated persistent binding of these compounds to Mpro, with RMSD values ranging from 0. 5 to 2. 0 nm, suggesting their potential as effective inhibitors. These findings suggest that the proposed ligands hold promise as potential scaffolds for developing potent antiviral drugs against COVID-19.

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Concepts Keywords
K36 3C-like proteinase, SARS-CoV-2
Molecular Antiviral Agents
Pandemic Antiviral Agents
Therapeutics Betacoronavirus
Viral Catalytic Domain
Coronavirus 3C Proteases
Coronavirus 3C Proteases
COVID-19
COVID-19 Drug Treatment
Humans
Molecular Docking Simulation
Molecular Dynamics Simulation
Pandemics
Protease Inhibitors
Protease Inhibitors
Protein Binding
SARS-CoV-2
Viral Nonstructural Proteins
Viral Nonstructural Proteins

Semantics

Type Source Name
pathway KEGG Viral replication
drug DRUGBANK Pentaerythritol tetranitrate
disease IDO site
disease MESH COVID-19
drug DRUGBANK Rasagiline
drug DRUGBANK Coenzyme M
disease MESH Long COVID
disease IDO production
drug DRUGBANK Chymotrypsin
drug DRUGBANK L-Cysteine
disease IDO cell
disease IDO replication
pathway REACTOME Release
disease IDO immune response
pathway REACTOME Immune System
disease IDO blood
disease MESH emergency
drug DRUGBANK Dexamethasone
drug DRUGBANK Oxygen
disease IDO protein
drug DRUGBANK Ritonavir
drug DRUGBANK Water
disease IDO algorithm
disease IDO process
drug DRUGBANK Gold
drug DRUGBANK Albendazole
drug DRUGBANK Eliglustat
drug DRUGBANK Eprazinone
drug DRUGBANK Amino acids
drug DRUGBANK Nitrogen
drug DRUGBANK Imidazole
drug DRUGBANK Isoxaflutole
disease IDO role
drug DRUGBANK Boceprevir
disease IDO organism
disease IDO history
disease MESH Infection
drug DRUGBANK Lopinavir
disease MESH multiple myeloma
disease IDO pathogen
disease IDO quality
disease MESH hiv infection
pathway REACTOME HIV Infection
pathway REACTOME Reproduction

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