Literature DB >> 27454620

Synthesis of pyrimidine-2,4,6-trione derivatives: Anti-oxidant, anti-cancer, α-glucosidase, β-glucuronidase inhibition and their molecular docking studies.

Assem Barakat1, Mohammad Shahidul Islam2, Abdullah Mohammed Al-Majid2, Hazem A Ghabbour3, Sammer Yousuf4, Mahwish Ashraf4, Nimra Naveed Shaikh4, M Iqbal Choudhary5, Ruqaiya Khalil6, Zaheer Ul-Haq6.   

Abstract

This paper describes a facile protocol, efficient, and environmentally benign for the synthesis a series of barbiturate acid substituted at C5 position 3a-o. The desired compounds subjected in vitro for different set of bioassays including against anti-oxidant (DPPH and super oxide scavenger assays), anti-cancer, α-glucosidase and β-glucuronidase inhibitions. Compound 3m (IC50=22.9±0.5μM) found to be potent α-glucosidase enzyme inhibitors and showed more activity than standard acarbose (IC50=841±1.73μM). Compound 3f (IC50=86.9±4.33μM) found to be moderate β-Glucuronidase enzyme inhibitors and showed activity comparatively less than the standard d-saccharic acid 1,4-lactone (IC50=45.75±2.16μM). Furthermore, in sillico investigation was carried out to investigate bonding mode of barbiturate acid derivatives.
Copyright © 2016 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Anti-cancer; Anti-oxidant; Pyrimidine-2,4,6-trione; α-Glucosidase inhibitor; β-Glucuronidase inhibitor

Mesh:

Substances:

Year:  2016        PMID: 27454620     DOI: 10.1016/j.bioorg.2016.07.009

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


  5 in total

1.  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

Review 2.  Therapeutic significance of β-glucuronidase activity and its inhibitors: A review.

Authors:  Paul Awolade; Nosipho Cele; Nagaraju Kerru; Lalitha Gummidi; Ebenezer Oluwakemi; Parvesh Singh
Journal:  Eur J Med Chem       Date:  2019-12-04       Impact factor: 6.514

3.  Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.

Authors:  Zipeng Gong; Zhenzhen Xie; Jie Qiu; Guangcheng Wang
Journal:  Molecules       Date:  2017-10-30       Impact factor: 4.411

4.  Synthesis and Inhibitory Effect of Some Indole-Pyrimidine Based Hybrid Heterocycles on α-Glucosidase and α-Amylase as Potential Hypoglycemic Agents.

Authors:  Farid A Badria; Saleh Atef; Abdullah Mohammed Al-Majid; M Ali; Yaseen A M M Elshaier; Hazem A Ghabbour; Mohammad Shahidul Islam; Assem Barakat
Journal:  ChemistryOpen       Date:  2019-10-22       Impact factor: 2.911

5.  Combinational therapeutics to combat cancer.

Authors:  Ahmed Al Otaibi; Subuhi Sherwani; Eida Mohammed Alshammari; Salma Ahmed Al-Zahrani; Wahid Ali Khan; Abdulmohsen Khalaf Dhahi Alsukaibi; Sourabh Dwivedi; Shahper Nazeer Khan; Mohd Wajid Ali Khan
Journal:  Bioinformation       Date:  2021-07-31
  5 in total

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