Literature DB >> 24927033

Design, synthesis and glucose uptake activity of some novel glitazones.

Koyel Kar1, Uma Krithika1, Prabhuddha Basu1, S Santhosh Kumar1, Anu Reji1, B R Prashantha Kumar2.   

Abstract

Herein, we report a library consisting of some novel glitazones containing thiazolidinedione and its bioisosteres, rhodanine and oxadiazolidine ring structures as their basic scaffold for their antidiabetic activity. Twelve novel glitazones with diverse chemical structures were designed and synthesized by adopting appropriate synthetic schemes and analyzed. Later, subjected to in vitro glucose uptake assay in the absence and presence of insulin to confirm their antidiabetic activity using rat hemi-diaphragm. The titled compounds exhibited glucose uptake activity ranging weak to significant activity. Compounds 4, 5, 9, 11, 15, 16, 19 and 20 showed considerable glucose uptake activity apart from rosiglitazone, a standard drug. Compound 16 happens to be the candidate compound from this study to investigate further. The illustration about their design, synthesis, analysis and glucose uptake activity is reported here along with the in vitro and in silico study based structure-activity relationships.
Copyright © 2014 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Glitazones; Glucose uptake activity; Rat hemi-diaphragm; Thiazolidinediones

Mesh:

Substances:

Year:  2014        PMID: 24927033     DOI: 10.1016/j.bioorg.2014.05.006

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


  5 in total

1.  Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies.

Authors:  Mohammed S Taghour; Hazem Elkady; Wagdy M Eldehna; Nehal M El-Deeb; Ahmed M Kenawy; Eslam B Elkaeed; Aisha A Alsfouk; Mohamed S Alesawy; Ahmed M Metwaly; Ibrahim H Eissa
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

2.  Novel Benzylidene Thiazolidinedione Derivatives as Partial PPARγ Agonists and their Antidiabetic Effects on Type 2 Diabetes.

Authors:  Sabina Yasmin; Fabio Capone; Antonio Laghezza; Fabrizio Dal Piaz; Fulvio Loiodice; Viswanathan Vijayan; Velmurugan Devadasan; Susanta K Mondal; Özlem Atlı; Merve Baysal; Ashok K Pattnaik; Venkatesan Jayaprakash; Antonio Lavecchia
Journal:  Sci Rep       Date:  2017-10-31       Impact factor: 4.379

3.  Synthesis and Antibacterial Activity of New Thiazolidine-2,4-dione-Based Chlorophenylthiosemicarbazone Hybrids.

Authors:  Nazar Trotsko; Urszula Kosikowska; Agata Paneth; Tomasz Plech; Anna Malm; Monika Wujec
Journal:  Molecules       Date:  2018-04-26       Impact factor: 4.411

4.  New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies.

Authors:  Eslam B Elkaeed; Mohammed S Taghour; Hazem A Mahdy; Wagdy M Eldehna; Nehal M El-Deeb; Ahmed M Kenawy; Bshra A Alsfouk; Mohammed A Dahab; Ahmed M Metwaly; Ibrahim H Eissa; Mohamed A El-Zahabi
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

5.  Design, synthesis, anti-proliferative evaluation, docking, and MD simulations studies of new thiazolidine-2,4-diones targeting VEGFR-2 and apoptosis pathway.

Authors:  Mohammed S Taghour; Hazem Elkady; Wagdy M Eldehna; Nehal El-Deeb; Ahmed M Kenawy; Eslam B Elkaeed; Bshra A Alsfouk; Mohamed S Alesawy; Dalal Z Husein; Ahmed M Metwaly; Ibrahim H Eissa
Journal:  PLoS One       Date:  2022-09-23       Impact factor: 3.752

  5 in total

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