Molecular diversity · 2024
Design, synthesis, and computational analysis (molecular docking, DFT, MEP, RDG, ELF) of diazepine and oxazepine sulfonamides: biological evaluation for in vitro and in vivo anti-inflammatory, antimicrobial, and cytotoxicity predictions.
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Hassan Sangar Ali, Aziz Dara Muhammed, Kader Dana Ali, Rasul Shwana Muhamad, Muhamad Meer Ali, Muhammedamin Alla Ahmad
Аннотация
We report the synthesis and extensive characterization of Diazepane and Oxazepane derivatives, followed by their biological evaluation. These compounds were assessed for in vitro and in vivo antimicrobial, anti-inflammatory, and anticancer activities. Among the synthesized molecules, compound 5b demonstrated remarkable antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis with MIC values of 20 and 40 μg/mL, respectively. Additionally, 5b exhibited potent anti-inflammatory effects both in vitro and in vivo. Advanced computational studies, including DFT, MEP, RDG, and ELF analyses, were performed to understand the electronic distribution and molecular interactions. The bioactivity and physicochemical properties of these derivatives were further predicted using PASS and pkCSM platforms, emphasizing their potential as promising lead molecules in drug development.
Предметные рубрики MeSH
Molecular Docking SimulationAzepinesAnti-Inflammatory AgentsDrug DesignSulfonamidesOxazepinesAnimalsAnti-Bacterial AgentsHumansMicrobial Sensitivity TestsAntineoplastic AgentsStaphylococcus aureusMiceDensity Functional TheoryStaphylococcus epidermidisAnti-Infective AgentsStructure-Activity Relationship