Review Article

药物化学领域含硼氨基酸的结构和生物学概述

卷 26, 期 26, 2019

页: [5077 - 5089] 页: 13

弟呕挨: 10.2174/0929867325666180926150403

价格: $65

摘要

背景:氨基酸是蛋白质的基本结构单元,也是许多具有生物活性的化合物的前体。据报道,硼的添加引起氨基酸化学生物学特性的改变。 方法:我们收集了有关某些化合物的生物学效应的信息,并讨论了添加硼的结构-活性关系。目前的重点是α-氨基酸的硼酸酯衍生物,由于添加含硼部分而引起的生物学活性的特定变化,以及鉴定一些有吸引力的化合物作为潜在的新药进行测试。 结果:α-氨基酸的硼酸酯衍生物已被广泛合成并作为潜在的新治疗工具进行了测试。 B-N(1.65 A°)或B-C(1.61 A°)或B-O(1.50 A°)键通常是这些化合物在不同pH和温度下的稳定性和活性的关键。合成衍生物的化学特征,例如特定部分和logP,硼原子的可极化性和位置,显然与其药效和药代动力学特征有关。已经提出或证明了某些作用机制,而对其他作用负责的机制尚不清楚。 结论:α-氨基酸的合成硼酸酯衍生物数量的增加以及最近报道的晶体结构为这些化合物在不同pH和温度下的稳定性,它们在药物靶标上的相互作用以及五个环的形成提供了新的见解。元杂环。需要进一步的研究来阐明实现特定合成的方法,所观察到的生物学效应所涉及的机制以及这种类型的含硼化合物(BCC)的毒理学特征。

关键词: 硼,氨基酸,构效关系,分配系数,药物设计,合成硼衍生物。

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