Literature DB >> 29169079

Design, synthesis and molecular docking of thiazolidinedione based benzene sulphonamide derivatives containing pyrazole core as potential anti-diabetic agents.

Mohd Javed Naim1, Ozair Alam2, Md Jahangir Alam1, Md Quamrul Hassan3, Nadeem Siddiqui1, V G M Naidu4, Md Iqbal Alam5.   

Abstract

We herein report the design, synthesis and molecular docking studies of 2,4-thiazolidinedione derivatives containing benzene sulphonyl group which are docked against the Peroxisome Proliferator Activated Receptor (PPARγ) target. Compound 7p was most effective in lowering the blood glucose level as compared to standard drugs pioglitazone and rosiglitazone. Compound 7p exhibited potent PPAR-γ transactivation of 61.2% with 1.9 folds increase in gene expression. In molecular docking studies 7p showed excellent interactions with amino acids TYR 473, SER 289, HIE 449, TYR 327, ARG 288, MET 329 and LEU 228. Compound 7p did not cause any damage to the liver without any noteworthy weight gain and may be considered as promising candidates for the development of new antidiabetic agents.
Copyright © 2017. Published by Elsevier Inc.

Entities:  

Keywords:  Anti-diabetic; Gene expression; Molecular docking; PPARγ; Pyrazole; Thiazolidinedione

Mesh:

Substances:

Year:  2017        PMID: 29169079     DOI: 10.1016/j.bioorg.2017.11.010

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


  7 in total

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Authors:  G Prashanth; Basavaraj Vastrad; Anandkumar Tengli; Chanabasayya Vastrad; Iranna Kotturshetti
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3.  Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors.

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Review 4.  Heterocyclic compounds as a magic bullet for diabetes mellitus: a review.

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Review 6.  An overview on medicinal perspective of thiazolidine-2,4-dione: A remarkable scaffold in the treatment of type 2 diabetes.

Authors:  Garima Bansal; Punniyakoti Veeraveedu Thanikachalam; Rahul K Maurya; Pooja Chawla; Srinivasan Ramamurthy
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7.  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
  7 in total

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