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2-噻吩巴比妥及其N-甲基衍生物在β-环糊精存在下的稳定性

Stability of 2-thiophenobarbital and its N-methyl derivatives in the presence of beta-cyclodextrin.

作者信息

Zuchowski Grzegorz, Tarsa Monika, Stasiewicz-Urban Anna, Bojarski Jacek

机构信息

Department of Organic Chemistry, Medical College, Jagiellonian University, Medyczna 9, 30-688 Kraków, Poland.

出版信息

Acta Pol Pharm. 2005 Sep-Oct;62(5):335-40.

PMID:16459481
Abstract

The rates of hydrolysis of thiophenobarbital and its N-mono- and N,N'-dimethyl-derivatives were determined under different conditions of pH and temperature using UV spectroscopy. They were compared with those obtained in the presence of different concentrations of beta-cyclodextrin. It was found that the compounds degrade with different rates and beta-cyclodextrin retards the hydrolysis. The formation of complexes between the investigated compounds and beta-cyclodextrin was proved by 13C NMR and ROESY spectra and molecular modeling. The inclusion with the phenyl substituent into the beta-cyclodextrin cavity is preferred.

摘要

使用紫外光谱法在不同的pH和温度条件下测定了硫喷妥钠及其N-单甲基和N,N'-二甲基衍生物的水解速率。将它们与在不同浓度的β-环糊精存在下获得的水解速率进行了比较。发现这些化合物以不同的速率降解,并且β-环糊精会延缓水解。通过13C NMR、ROESY光谱和分子模拟证明了所研究的化合物与β-环糊精之间形成了复合物。苯基取代基优先包合进入β-环糊精空腔。

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