| Literature DB >> 29169079 |
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.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