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Biochemistry, Biophysics, and Structural Biology Commons

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2020

Articles

Aryl piperazine

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Full-Text Articles in Biochemistry, Biophysics, and Structural Biology

Characterization Of An Aryl Piperazine/2-Hydroxypropyl-Β-Cyclodextrin Association, A Complex With Antidiabetic Potential, R. Devine, D.S.D. Martin, Gemma Kinsella, J.B.C. Findlay, J.C. Stephens Jan 2020

Characterization Of An Aryl Piperazine/2-Hydroxypropyl-Β-Cyclodextrin Association, A Complex With Antidiabetic Potential, R. Devine, D.S.D. Martin, Gemma Kinsella, J.B.C. Findlay, J.C. Stephens

Articles

This study explores the molecular association between 4-(thiophen-2-yl)-1-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)butan-1-one (RTC1), an antidiabetic compound recently reported by our research group with challenging aqueous solubility, and 2-hydroxypropyl-β-cyclodextrin (HPBCD). The formation of a RTC1/HPBCD complex resulted in improved solubility. A phase-solubility diagram was used to determine the complex stability constant and stoichiometric ratio. 2D 1H NMR spectroscopy was utilized to study the molecular interaction between RTC1 and HPBCD in the complex. Differential scanning calorimetry and scanning electron microscopy was also employed to confirm complex formation. In vitro biological evaluation, using a glucose uptake assay, showed that the homogeneous RTC1/HPBCD complex solution showed the …