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

被引:0
|
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;
D O I
暂无
中图分类号
学科分类号
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.
引用
收藏
页码:2441 / 2454
页数:13
相关论文
共 50 条
  • [31] Synthesis, crystal structure and β-glucuronidase inhibition activity of some new hydrazinecarboxamides and their 1,2,4-triazole derivatives
    Hanif, Muhammad
    Khan, Imtiaz
    Rama, Nasim Hasan
    Noreen, Shagufta
    Choudhary, Muhammad Iqbal
    Jones, Peter G.
    Iqbal, Mazhar
    MEDICINAL CHEMISTRY RESEARCH, 2012, 21 (11) : 3885 - 3896
  • [32] Novel 1,2,4-triazole derivatives: Design, synthesis, anticancer evaluation, molecular docking, and pharmacokinetic profiling studies
    Turky, Abdallah
    Sherbiny, Farag F.
    Bayoumi, Ashraf H.
    Ahmed, Hany E. A.
    Abulkhair, Hamada S.
    ARCHIV DER PHARMAZIE, 2020, 353 (12)
  • [33] A biochemistry-oriented drug design: synthesis, anticancer activity, enzymes inhibition, molecular docking studies of novel 1,2,4-triazole derivatives
    Yuriy, Karpenko
    Kusdemir, Gulnur
    Volodymyr, Parchenko
    Tuzun, Burak
    Taslimi, Parham
    Karatas, Omer Faruk
    Anastasia, Khilkovets
    Maryna, Parchenko
    Sayin, Koray
    JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2024, 42 (03): : 1220 - 1236
  • [34] New 1,2,4-Triazole Scaffolds as Anticancer Agents: Synthesis, Biological Evaluation and Docking Studies
    Maddali, Narendra Kumar
    Ivaturi, V. Kasi Viswanath
    Murthy Yellajyosula, L. N.
    Malkhed, Vasavi
    Brahman, Pradeep Kumar
    Pindiprolu, Sai Kiran S. S.
    Kondaparthi, Vani
    Nethinti, Sundara Rao
    CHEMISTRYSELECT, 2021, 6 (26): : 6788 - 6796
  • [35] Synthesis, characterization, and biological activity of novel 1,2,4-triazole moieties: Antileishmanial, antimicrobial effects, and molecular docking studies
    Suleymanoglu, Nevin
    Unver, Yasemin
    Ustabas, Resat
    Celik, Fatih
    Guler, Halil Ibrahim
    Direkel, Sahin
    Bektas, Kadriye Inan
    JOURNAL OF MOLECULAR STRUCTURE, 2024, 1314
  • [36] Molecular docking studies, biological evaluation and synthesis of novel 3-mercapto-1,2,4-triazole derivatives
    Ghanaat, Javad
    Khalilzadeh, Mohammad A.
    Zareyee, Daryoush
    MOLECULAR DIVERSITY, 2021, 25 (01) : 223 - 232
  • [37] SYNTHESIS OF 2,5-DIBROMO-1,2,4-TRIAZOLE BY BROMINATION OF 1,2,4-TRIAZOLE [1]
    KROGER, CF
    FRANK, H
    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 1965, 4 (05) : 434 - &
  • [38] Molecular docking studies, biological evaluation and synthesis of novel 3-mercapto-1,2,4-triazole derivatives
    Javad Ghanaat
    Mohammad A. Khalilzadeh
    Daryoush Zareyee
    Molecular Diversity, 2021, 25 : 223 - 232
  • [39] Synthesis of 1,2,4-triazole dendrimers
    Maes, W
    Verstappen, B
    Dehaen, W
    TETRAHEDRON, 2006, 62 (11) : 2677 - 2683
  • [40] STUDIES ON MECHANISM OF INHIBITION OF SALMONELLA-TYPHIMURIUM BY 1,2,4-TRIAZOLE
    KREDICH, NM
    FOOTE, LJ
    HULANICKA, MD
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1975, 250 (18) : 7324 - 7331