Literature DB >> 29454828

Evaluation of α-glucosidase inhibiting potentials with docking calculations of synthesized arylidene-pyrazolones.

Faryal Chaudhry1, Sadia Naureen2, Shahnaz Choudhry3, Rahila Huma4, Muhammad Ashraf5, Mariya Al-Rashida6, Bakhat Jahan5, Masooma Hyder Khan4, Farah Iqbal4, Munawar Ali Munawar7, Misbahul Ain Khan8.   

Abstract

Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones 2(a-d) lead to the corresponding arylidene-pyrazolones 3(a-l) which were tested against α-glucosidase enzyme. The synthesized compounds displayed moderate to good activity. Among these, a coumarin derivative 3k exhibited excellent results (IC50 2.10 ± 0.004 µM) in comparison to clinical drug acarbose (IC50 37.38 ± 0.12 µM). The ligand-protein interactions were identified through docking and stabilizing energy calculations.
Copyright © 2018 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Antipyrine; Arylidenes; Coumarins; Enzyme Inhibitor; Knoevenagel condensations

Mesh:

Substances:

Year:  2018        PMID: 29454828     DOI: 10.1016/j.bioorg.2018.02.002

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


  4 in total

1.  Design and synthesis of new imidazo[1,2-b]pyrazole derivatives, in vitro α-glucosidase inhibition, kinetic and docking studies.

Authors:  Fariba Peytam; Mehdi Adib; Reihaneh Shourgeshty; Maryam Mohammadi-Khanaposhtani; Mehdi Jahani; Somaye Imanparast; Mohammad Ali Faramarzi; Mohammad Mahdavi; Ali Akbar Moghadamnia; Hossein Rastegar; Bagher Larijani
Journal:  Mol Divers       Date:  2019-03-02       Impact factor: 2.943

2.  A novel series of mixed-ligand M(II) complexes containing 2,2'-bipyridyl as potent α-glucosidase inhibitor: synthesis, crystal structure, DFT calculations, and molecular docking.

Authors:  Davut Avcı; Sümeyye Altürk; Fatih Sönmez; Ömer Tamer; Adil Başoğlu; Yusuf Atalay; Belma Zengin Kurt; Necmi Dege
Journal:  J Biol Inorg Chem       Date:  2019-07-17       Impact factor: 3.358

3.  An efficient and targeted synthetic approach towards new highly substituted 6-amino-pyrazolo[1,5-a]pyrimidines with α-glucosidase inhibitory activity.

Authors:  Fariba Peytam; Mehdi Adib; Reihaneh Shourgeshty; Loghman Firoozpour; Mahmoud Rahmanian-Jazi; Mehdi Jahani; Setareh Moghimi; Kouros Divsalar; Mohammad Ali Faramarzi; Somayeh Mojtabavi; Fatemeh Safari; Mohammad Mahdavi; Alireza Foroumadi
Journal:  Sci Rep       Date:  2020-02-13       Impact factor: 4.379

4.  Pyrazolo[4,3-c]pyridine Sulfonamides as Carbonic Anhydrase Inhibitors: Synthesis, Biological and In Silico Studies.

Authors:  Andrea Angeli; Victor Kartsev; Anthi Petrou; Boris Lichitsky; Andrey Komogortsev; Mariana Pinteala; Athina Geronikaki; Claudiu T Supuran
Journal:  Pharmaceuticals (Basel)       Date:  2022-03-07
  4 in total

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