期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 8, 期 4, 页码 765-773出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/b918372h
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资金
- EPSRC [EP/E036244/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/E036244/1] Funding Source: researchfish
The inclusion of the cardiovascular beta-blocker drug atenolol, the antidiabetic drug glibenclamide, the Alzheimer's NMDA glutamate receptor drug memantine and the analgesic/antipyretic drug paracetamol by cucurbit[7]uril (CB[7]) has been studied by H-1 nuclear magnetic resonance spectroscopy, electrospray ionisation mass spectrometry, molecular modelling, fluorescence displacement assays and differential scanning calorimetry. All four drugs form 1 : 1 host-guest complexes with CB[7], but the exchange kinetics and location of the binding is different for each drug. Atenolol is bound over the central phenyl ring with a binding constant of 4.2 x 10(4) M-1, whereas glibenclamide is bound over the terminal cyclohexyl group with a binding constant of 1.7 x 10(5) M-1, and memantine is totally bound within the CB[7]cavity. Paracetamol is bound in two locations, over the central phenyl ring and over the methyl group, with the CB[7]molecule shuttling quickly between the two sites. Inclusion by CB[7]was shown by differential scanning calorimetry to physically stabilise all four drugs, which has applications preventing drug degradation and improving drug processing and formulation.
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