Synthesis, β-Glucuronidase Inhibition, and Molecular Docking Studies of 1,2,4-Triazole Hydrazones

被引:0
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作者
Waqas Jamil
Darshana Kumari
Muhammad Taha
Muhammad Naseem Khan
Mohd Syukri Baharudin
Muhammad Ali
M. Kanwal
Muhammad Saleem Lashari
Khalid Muhammad Khan
机构
[1] University of Sindh,Institute of Advance Research Studies in Chemical Sciences
[2] Imam Abdul Rehman Bin Faisal University,Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC)
[3] University Road,Department of Chemistry, COMSATS Institute of Information Technology
[4] Universiti Teknologi MARA (UiTM),Atta
[5] University of Karachi,ur
[6] University of Education,Rahman Institute for Natural Product Discovery
[7] University of Nizwa,H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences
关键词
1,2,4-Triazole hydrazone; -Glucuronidase enzyme inhibition; Anti-diabetic; In silico studies;
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摘要
A series of 1,2,4-triazole hydrazones 1–25 has been synthesized and characterized using different spectroscopic techniques including FT-IR, 1H-NMR, and ESI MS spectrometry. The synthetic derivatives were evaluated for their β-glucuronidase enzyme inhibition properties. Among them, 17 compounds demonstrated potential inhibitory activity towards β-glucuronidase with IC50 values ranging between 2.50 and 53.70 µM. Compounds 1 having IC50 = 2.50 ± 0.01 µM was found to be the most active compound of the series and showed remarkable activity and found to be far more potent than the standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 µM). Furthermore, the possible binding interaction of active compounds was explored by in silico studies. These compounds can be used for anti-diabetic drug development process.
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页码:2441 / 2454
页数:13
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