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040 _aAIKTC-KRRC
_cAIKTC-KRRC
100 _914731
_a Mehta, Mukul
245 _aSynthesis and Anti-hyperglycaemic Study of Aryl Sulfonate Ester Conjugated 5-arylidene-thiazolidine-2,4-diones
250 _aVol.55(3), Jul-Sep
260 _aBanagalore
_bAssociation of Pharmaceutical Teachers of India (APTI)
_c2021
300 _a894-903p.
520 _aBackground: Diabetes mellitus, a lifestyle related global health crisis has rapidly engulfed the entire world. In the past, various thiazolidinedione derivatives have been successfully developed for management of diabetes. Materials and Methods: Herein, we report synthesis, characterization (1H-NMR, 13C-NMR and mass spectroscopy methods) of novel aryl sulfonyloxy-5-arylidene thiazolidine-2,4-dione analogues. Anti-hyperglycaemic action (Alloxan-induced method) was performed for evaluating the antidiabetic potential of the synthesized compounds. Docking analysis of the final compounds were carried out to reveal interactions with the active site pocket of enzymes like protein tyrosine phosphatase 1B, aldose reductase and peroxisome proliferator activated-γ. The synthesized compounds were further subjected to ADME (Absorption, Distribution, Metabolism, Elimination) prediction studies to prove their drug-like potential. Results: Compound 10 and 12 showed comparable reduction in blood sugar as that with pioglitazone. Docking studies helped in understanding the probable binding mode inside the binding cavity of the concerned receptors. Conclusion: Aryl sulfonate esters with phenyl and chloro phenyl substituents were found to have superior anti-hyperglycaemic activity.
650 0 _94639
_aPHARMACEUTICS
700 _914732
_aMahapatra, Manoj Kumar
773 0 _dBengluru Association of Pharmaceutical Teachers of India (APTI)
_x0019-5464
_tIndian journal of pharmaceutical education and research
856 _uhttps://www.ijper.org/sites/default/files/IndJPhaEdRes-55-3-894.pdf
_yClick here
942 _2ddc
_cAR