Literature DB >> 30396060

Imidazole-pyrazole hybrids: Synthesis, characterization and in-vitro bioevaluation against α-glucosidase enzyme with molecular docking studies.

Faryal Chaudhry1, Sadia Naureen2, Muhammad Ashraf3, Mariya Al-Rashida4, Bakhat Jahan3, Munawar Ali Munawar5, Misbahul Ain Khan6.   

Abstract

Herein, substituted imidazole-pyrazole hybrids (2a-2n) were prepared via a multi component reaction employing pyrazole-4-carbaldehydes (1a-1d), ammonium acetate, benzil and arylamines as reactants. All the new compounds were characterized through their spectral and elemental analyses. Further these compounds were tested against α-glucosidase enzyme. The compounds 2k, 2l and 2n possessed good inhibition potencies, however, compounds 2f (IC50 value: 25.19 ± 0.004 μM) and 2m (IC50 value: 33.62 ± 0.03 μM) were the most effective compounds of the series. Furthermore, molecular docking helped to understand the binding interactions of 2f and 2m with the understudy yeast's α-glucosidase enzyme.
Copyright © 2018 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Molecular modeling; Multicomponent reactions; Tetrasubstituted imidazoles; α-Glucosidase inhibitors

Mesh:

Substances:

Year:  2018        PMID: 30396060     DOI: 10.1016/j.bioorg.2018.10.047

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  6 in total

Review 1.  Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives.

Authors:  Diana Becerra; Rodrigo Abonia; Juan-Carlos Castillo
Journal:  Molecules       Date:  2022-07-23       Impact factor: 4.927

2.  Synthesis and Biological Evaluation of 5-Fluoro-2-Oxindole Derivatives as Potential α-Glucosidase Inhibitors.

Authors:  Jing Lin; Qi-Ming Liang; Yuan-Na Ye; Di Xiao; Li Lu; Meng-Yue Li; Jian-Ping Li; Yu-Fei Zhang; Zhuang Xiong; Na Feng; Chen Li
Journal:  Front Chem       Date:  2022-06-23       Impact factor: 5.545

3.  Antimicrobial screening to molecular docking of newly synthesized ferrocenyl-substituted pyrazole.

Authors:  Shashi Sharma; Hardeep Singh Tuli; Mehmet Varol; Pallvi Agarwal; Anita Rani; Zahoor Abbas; Manoj Kumar
Journal:  Int J Health Sci (Qassim)       Date:  2022 Jul-Aug

4.  Design, Synthesis, Anticancer Evaluation, Enzymatic Assays, and a Molecular Modeling Study of Novel Pyrazole-Indole Hybrids.

Authors:  Ashraf S Hassan; Gaber O Moustafa; Hanem M Awad; Eman S Nossier; Mohamed F Mady
Journal:  ACS Omega       Date:  2021-04-29

Review 5.  A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications.

Authors:  Nagaraju Kerru; Lalitha Gummidi; Suresh Maddila; Kranthi Kumar Gangu; Sreekantha B Jonnalagadda
Journal:  Molecules       Date:  2020-04-20       Impact factor: 4.411

6.  Synthesis, Crystal Structures, and Density Functional Theory Studies of Two Salt Cocrystals Containing Meldrum's Acid Group.

Authors:  Wulan Zeng; Xia Wang; Yunju Zhang
Journal:  ACS Omega       Date:  2022-07-13
  6 in total

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