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Synthesis, In Silico And Pharmacological Evaluation Of New Thiazolidine-4-Carboxylic Acid Derivatives Against Ethanol-Induced Neurodegeneration And Memory Impairment, Shagufta Naz, Lina Tariq Al Kury, Humaira Nadeem, Fawad Ali Shah, Rehan Zafar Paracha, Muhammad Imran, Shupeng Li, Aman Ullah Jan 2022

Synthesis, In Silico And Pharmacological Evaluation Of New Thiazolidine-4-Carboxylic Acid Derivatives Against Ethanol-Induced Neurodegeneration And Memory Impairment, Shagufta Naz, Lina Tariq Al Kury, Humaira Nadeem, Fawad Ali Shah, Rehan Zafar Paracha, Muhammad Imran, Shupeng Li, Aman Ullah

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Introduction: Several studies revealed that alcohol utilization impairs memory in adults; however, the underlying mechanism is still unclear. The production of inflammatory markers and reactive oxygen species (ROS) plays a major role in neurodegeneration, which leads to memory impairment. Therefore, targeting neuroinflammation and oxidative distress could be a useful strategy for abrogating the hallmarks of ethanol-induced neurodegeneration. Moreover, several studies have demonstrated multiple biological activities of thiazolidine derivatives including neuroprotection. Methods: In the current study, we synthesized ten (10) new thiazolidine-4-carboxylic acid derivatives (P1-P10), characterized their synthetic properties using proton nuclear magnetic resonance (1 H-NMR) and carbon-13 NMR, and further …


Benzimidazole Derivatives As New Potential Nlrp3 Inflammasome Inhibitors That Provide Neuroprotection In A Rodent Model Of Neurodegeneration And Memory Impairment, Aman Ullah, Lina Tariq Al Kury, Yusuf S. Althobaiti, Tahir Ali, Fawad Ali Shah Jan 2022

Benzimidazole Derivatives As New Potential Nlrp3 Inflammasome Inhibitors That Provide Neuroprotection In A Rodent Model Of Neurodegeneration And Memory Impairment, Aman Ullah, Lina Tariq Al Kury, Yusuf S. Althobaiti, Tahir Ali, Fawad Ali Shah

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Objective: The study investigated the effect of newly synthesized benzimidazole derivatives against ethanol-induced neurodegenera-tion. According to evidence, ethanol consumption may cause a severe insult to the central nervous system (CNS), resulting in mental retardation, neuronal degeneration, and oxidative stress. Targeting neuroinflammation and oxidative stress may be a useful strategy for preventing ethanol-induced neurodegeneration. Methodology: Firstly, the newly synthesized compounds were subjected to molecular simulation and docking in order to predict ligand binding status. Later, for in vivo observations, adult male Sprague Dawley rats were used for studying behavioral and oxidative stress markers. ELIZA kits were used to analyse tumour necrosis …


Neuroprotective Effects Of Melatonin And Celecoxib Against Ethanol-Induced Neurodegeneration: A Computational And Pharmacological Approach, Lina T. Al Kury, Alam Zeb, Zain Ul Abidin, Nadeem Irshad, Imran Malik, Arooj Mohsin Alvi, Atif Ali Khan Khalil, Sareer Ahmad, Muhammad Faheem, Arif Ullah Khan, Fawad Ali Shah, Shupeng Li Jan 2019

Neuroprotective Effects Of Melatonin And Celecoxib Against Ethanol-Induced Neurodegeneration: A Computational And Pharmacological Approach, Lina T. Al Kury, Alam Zeb, Zain Ul Abidin, Nadeem Irshad, Imran Malik, Arooj Mohsin Alvi, Atif Ali Khan Khalil, Sareer Ahmad, Muhammad Faheem, Arif Ullah Khan, Fawad Ali Shah, Shupeng Li

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© 2019 Al Kury et al. This work is published and licensed by Dove Medical Press Limited. Purpose: Melatonin and celecoxib are antioxidants and anti-inflammatory agents that exert protective effects in different experimental models. In this study, the neuroprotective effects of melatonin and celecoxib were demonstrated against ethanol-induced neuronal injury by in silico, morphological, and biochemical approaches. Methods: For the in silico study, 3-D structures were constructed and docking analysis performed. For in vivo studies, rats were treated with ethanol, melatonin, and celecoxib. Brain samples were collected for biochemical and morphological analysis. Results: Homology modeling was performed to build 3-D …