Discovery of new 2-(3-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl)thiazole derivatives with potential analgesic and anti-inflammatory activities: In vitro, in vivo and in silico investigations

Mohammed, Eman R.; Abd-El-Fatah, Aliaa H.; Mohamed, Abdalla R.; Mahrouse, Marianne A.; Mohammad, Mohammad A.

doi:10.1016/j.bioorg.2024.107372

Bioorganic Chemistry

2024

DOI: 10.1016/j.bioorg.2024.107372

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Discovery of new 2-(3-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl)thiazole derivatives with potential analgesic and anti-inflammatory activities: In vitro, in vivo and in silico investigations

Eman R. Mohammed,

Aliaa H. Abd-El-Fatah,

Abdalla R. Mohamed

et al.

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Cited by 3 publications

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Insight into the therapeutic potential of pyrazole‐thiazole hybrids: A comprehensive review

Sumran,

Sharma,

Aggarwal

2024

Archiv der Pharmazie

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Several pyrazole‐thiazole hybrids featuring two potentially bioactive pharmacophores with or without linker have been synthesized using the molecular hybridization approach as target structures by medicinal chemists to modulate multiple drug targets simultaneously. The presented review aims to provide an overview of the diversified and wide array of pharmacological activities of these hybrids bestowing anticancer, antifungal, antibacterial, analgesic, anti‐inflammatory, antioxidant, antitubercular, antiviral, antiparasitic, and miscellaneous activities. The structure–activity relationships and potential mechanism of action are also reviewed to shed light on the development of more effective and biotargeted candidates. This review focuses on the latest research advances in the biological profile of pyrazole‐thiazole hybrids reported from 2015 to the present, providing medicinal researchers with a comprehensive platform to rationally design and develop more promising pyrazole‐thiazole hybrids.

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Insight into the therapeutic potential of pyrazole‐thiazole hybrids: A comprehensive review

Sumran,

Sharma,

Aggarwal

2024

Archiv der Pharmazie

View full text Add to dashboard Cite

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Synthesis and Molecular Docking of Curcumin‐Derived Pyrazole‐Thiazole Hybrids as Potent α‐Glucosidase Inhibitors

Al‐Humaidi,

Albedair,

Maliwal

et al. 2024

Chemistry & Biodiversity

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α Glucosidase inhibitors are critical for diabetes management, with pyrazoles and thiazoles emerging as effective options. This research highlights curcumin‐based pyrazole‐thiazole hybrids as potential inhibitors, synthesizing derivatives and evaluating their inhibitory capabilities. The study involved the synthesis of novel compounds using hydrazonoyl halides, confirmed through elemental and spectral analyses. The synthesized derivatives exhibited significant α‐glucosidase inhibition, with IC50 values ranging from 3.37 ± 0.25 to 16.35 ± 0.37 µM. Among them, compound 7e demonstrated the strongest inhibition at 3.37 ± 0.25 µM, outperforming the standard drug acarbose (IC50 = 5.36 ± 0.31 µM). In silico assessments and molecular docking using AutoDock Vina revealed strong interactions, particularly with compounds 7b, 7e, 7f, and 7g, indicating their potential as stable and effective inhibitors. The results suggest that the synthesized pyrazole‐thiazole hybrids hold promise as novel therapeutic agents for diabetes, warranting further exploration of their substituent effects for optimized inhibitor design.

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Evaluation of the antifungal activity of novel bis-pyrazole carboxamide derivatives and preliminary investigation of the mechanism

Song,

Gao,

Wang

et al. 2024

Bioorganic Chemistry

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Discovery of new 2-(3-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl)thiazole derivatives with potential analgesic and anti-inflammatory activities: In vitro, in vivo and in silico investigations

Cited by 3 publications

References 53 publications

Insight into the therapeutic potential of pyrazole‐thiazole hybrids: A comprehensive review

Insight into the therapeutic potential of pyrazole‐thiazole hybrids: A comprehensive review

Synthesis and Molecular Docking of Curcumin‐Derived Pyrazole‐Thiazole Hybrids as Potent α‐Glucosidase Inhibitors

Evaluation of the antifungal activity of novel bis-pyrazole carboxamide derivatives and preliminary investigation of the mechanism

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