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DOI 10.1016/j.bioorg.2024.107761

Медицинская библиотека · Bioorganic chemistry · 2024

Discovery of new molecular hybrid derivatives with coumarin scaffold bearing pyrazole/oxadiazole moieties: Molecular docking, POM analyses, in silico pharmacokinetics and in vitro antimicrobial evaluation with identification of potent antitumor pharmacophore sites.

Tataringa Gabriela, Tuchilus Cristina, Ahmed Mukhtar, Ahmed Sumeer, Bhat Ajmal R, Ben Hadda Taibi, Zbancioc Ana-Maria, Fahelelbom Khairi M

СтатьяПоддержка исследования: вне правительства СШАПеревод пока не подготовлен

Аннотация

This synthetic organic methodology involves the creation of novel coumarin-based hybrids of series (1-4) with pyrazole ring and (5-8) with oxadiazole moiety. The targeted compounds were tested for In vitro Antimicrobial efficacy against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans pathogenic microbes using disc diffusion and broth microdilution with ciprofloxacin and fluconazole as reference standards. Density functional theory (DFT) studies were used to study atomic structure and reactivity, including absolute electronegativity (χ), electrophilicity (ω), electron acceptor (ω+), donor capabilities (ω-), electron affinity (EA), energy gap (ΔE), global hardness (η), global softness (S), and ionisation potential (IP) and FMOs, NBOs, MEP, and Mulliken Charge analysis. The POM tests found three integrated pharmacophore sites with antibacterial, antiviral, and anticancer activities. Molecular docking studies are also used to determine the S. aureus nucleoside diphosphate kinase receptor's affinity and mode of action for the synthesized drugs. In silico analysis of thermodynamic and therapeutic effectiveness properties, including Lipinski's 'rule of five', Veber's rule, and ADME properties, predicted toxicity-free, non-carcinogenic, and risk-free oral administration of the synthesized complexes.

Для цитирования: Tataringa Gabriela, Tuchilus Cristina, Ahmed Mukhtar, Ahmed Sumeer, Bhat Ajmal R, Ben Hadda Taibi, Zbancioc Ana-Maria, Fahelelbom Khairi M. Discovery of new molecular hybrid derivatives with coumarin scaffold bearing pyrazole/oxadiazole moieties: Molecular docking, POM analyses, in silico pharmacokinetics and in vitro antimicrobial evaluation with identification of potent antitumor pharmacophore sites.. Bioorganic chemistry. 2024. DOI: 10.1016/j.bioorg.2024.107761.

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