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Review Article

二肽基肽酶IV抑制剂开发的最新药物化学方法

卷 28, 期 18, 2021

发表于: 12 October, 2020

页: [3595 - 3621] 页: 27

弟呕挨: 10.2174/0929867327666201012153255

价格: $65

摘要

背景：糖尿病是一种代谢性疾病，因胰岛素降低或不影响血糖水平而发生。目前口服药物刺激胰岛素释放，增加葡萄糖吸收和利用，降低肝脏葡萄糖输出。两种主要肠促胰岛素激素如葡萄糖依赖的促胰岛素多肽(GIP)和胰高血糖素样肽-1 (GLP-1)刺激饭后胰岛素的释放，但它们的作用被二肽基肽酶- IV所抑制。 目的：内源性GLP-1和GIP的活性随着DPP IV抑制剂的增加而延长，DPP IV抑制剂负责刺激胰岛素分泌和调节血糖水平。DPP IV抑制剂已显示出有效性和耐受性，在2型糖尿病的管理中，对体重的中性影响以及低血糖的机会更少。这些旅程从Sitagliptin(2006年上市)开始，到Evogliptin(2015年上市，韩国)。 结论：2型糖尿病的治疗包括生活方式的改变，口服药物和胰岛素。与目前的处方药相比，更需要更新和更优越的疗法。人们已经尝试了各种杂环衍生物，但由于对DASH蛋白、CYP酶和hERG通道的掩盖，它们显示出了副作用。在此基础上，研究的重点是开发安全、有影响、选择性和长效的DPP IV抑制剂。

关键词: 糖尿病，DPP IV抑制剂，GLP -1，杂环衍生物，2型糖尿病，CYP酶

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