Permeability of novel 4′-N-substituted (aminomethyl) benzoate-7-substituted nicotinic acid ester derivatives of scutellarein in Caco-2 cells and in an in vitro model of the blood-brain barrier

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• 作者：Yu Ou ; Min Luo ; Yong-Xi Dong ; Hang Su ; Xiao-Zhong Fu…
• 关键词：Scutellarein ; Nicotinic acid ; Caco ; 2 cell ; Permeability ; In vitro blood–brain barrier model
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：25
• 期：10
• 页码：2205-2213
• 全文大小：551 KB
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120
• 卷排序：25

文摘

A series of 4′-N-substituted (aminomethyl) benzoate-7-substituted nicotinic acid ester derivatives of scutellarein was designed and synthesized. Evaluation of physiochemical properties showed that the newly designed compounds had greater chemical stability and aqueous solubility than scutellarin or scutellarein. The permeabilities (P_{app AP to BL}) of compounds 7b and 7e in Caco-2 cells were 5.9-fold and 3.7-fold higher than that of scutellarin, and 3.7-fold and 2.4-fold higher than that of scutellarein. The permeabilities (P_{app AP to BL}) of compounds 7b and 7e in an in vitro model of the blood–brain barrier were 9.7-fold and 5.9-fold higher than that of scutellarin, and 9.2-fold and 5.6-fold higher than that of scutellarein.