Litcius/Paper detail

Synthesis of New Organoselenium-Based Succinanilic and Maleanilic Derivatives and In Silico Studies as Possible SARS-CoV-2 Main Protease Inhibitors

Saad Shaaban, Yasair S. Al‐Faiyz, Ghayah M. Alsulaim, Mohamed Alaasar, Nasser Amri, Hussein Ba‐Ghazal, Ahmed A. Al‐Karmalawy, Aly Abdou

2023Inorganics65 citationsDOIOpen Access PDF

Abstract

Herein we report the synthesis of organic selenide-based maleanilic and succinanilic acids in good yields (up to 95%). Their structural identities were elucidated by spectroscopic techniques (e.g., IR, 1H- & 13C-NMR, and MS). The ADMET analysis, molecule electrostatic potential map, DFT, and frontier molecular orbital were used to study the organoselenium compounds’ pharmacokinetics, drug-likeness characteristics, geometries, and chemical and electronic properties. Moreover, a molecular docking tool was employed to investigate the organic selenides’ ability to inhibit the SARS-CoV-2 Mpro target (PDB: 7BFB). Within this context, organic selenides exhibited promising binding affinities to the SARS-CoV-2 Mpro receptor in the following order (12 > 11 > 10 > 9 > 7 > 8). Furthermore, molecular dynamics simulations were also carried out for 200 ns to evaluate the exact behavior of the most active compound (12) within the Mpro binding pocket of SARS-CoV-2 compared with its co-crystallized inhibitor (Co).

Topics & Concepts

ChemistryProtein Data Bank (RCSB PDB)Binding affinitiesIn silicoStereochemistryAffinitiesContext (archaeology)Molecular modelDocking (animal)Combinatorial chemistryMoleculeBiochemistryReceptorOrganic chemistryBiologyPaleontologyNursingGeneMedicineSynthesis and biological activityComputational Drug Discovery MethodsCholinesterase and Neurodegenerative Diseases