Synthesis of highly functionalized barbituric acids and study of their interactions with p-glycoprotein and Mg²⁺ – Potential candidates for multi drug resistance modulation

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• 作者：Palwinder Singh ; Jatinder Kaur ; Atul Bhardwaj
• 关键词：P-Glycoprotein ; Multi drug resistance ; Barbituric acid ; Docking
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：March 2010
• 年：2010
• 卷：45
• 期：3
• 页码：1256-1262
• 全文大小：928 K

文摘

A number of barbituric acids with appropriate substituent at C-5 position were synthesized and investigated for their interactions with p-gp and Mg²⁺. Compounds 5, 6, 8–10, 12–14 and 16 increased the basal activity of p-gp by more than 50 % at 0.05 μM concentration. Molecular docking indicate a number of H-bond interactions between these molecules and the amino acid residues of ATP binding site of p-gp. These molecules also showed appreciable interactions with Mg²⁺, an important component of efflux pump. All the results of these investigations favor the suitability of barbituric acids toward MDR modulation.