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临床可行的α-淀粉酶抑制剂开发中的关键分子支架

Key molecular scaffolds in the development of clinically viable α-amylase inhibitors.

作者信息

Singh Rahul, Sindhu Jayant, Singh Devender, Kumar Parvin

机构信息

Department of Chemistry, Kurukshetra University, Kurukshetra, India.

School of Chemistry, Indian Institutes of Science Education and Research, Thiruvananthapuram, India.

出版信息

Future Med Chem. 2025 Feb;17(3):347-362. doi: 10.1080/17568919.2025.2453421. Epub 2025 Jan 21.

DOI:10.1080/17568919.2025.2453421
PMID:39835704
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11792802/
Abstract

The escalating cases of type II diabetes combined with adverse side effects of current antidiabetic drugs spurred the advancement of innovative approaches for the management of postprandial glucose levels. α-Amylase is an endoamylase responsible for the breakdown of internal α-1,4-glycosidic linkages in dietary starch, producing oligosaccharides. Subsequently, α-glucosidase degraded these oligosaccharides to monosaccharides, which are absorbed into the bloodstream and become available to the body. The inhibitors of α-amylase reduced the digestibility of carbohydrates accompanied by delayed glucose absorption, leading to decreased blood glucose levels after meals and thus, inhibition of the enzyme seems to be a crucial strategy for diabetes management and improving overall glycemic control in diabetic patients. The present review article emphasizes the therapeutic promise of recently discovered potential α-amylase inhibitors, highlighting their , and profiles. Ultimately, we addressed the contemporary challenges and potential routes ahead in the search for safe and reliable α-amylase inhibitors for clinical use, summarizing the most recent research in the field.

摘要

II型糖尿病病例不断增加,加上现有抗糖尿病药物的不良副作用,促使人们开发创新方法来管理餐后血糖水平。α-淀粉酶是一种内切淀粉酶,负责分解膳食淀粉中的内部α-1,4-糖苷键,产生寡糖。随后,α-葡萄糖苷酶将这些寡糖降解为单糖,单糖被吸收进入血液并供身体利用。α-淀粉酶抑制剂降低了碳水化合物的消化率,同时延缓了葡萄糖吸收,导致餐后血糖水平降低,因此,抑制该酶似乎是糖尿病管理和改善糖尿病患者整体血糖控制的关键策略。本综述文章强调了最近发现的潜在α-淀粉酶抑制剂的治疗前景,突出了它们的 、 和 概况。最终,我们探讨了寻找安全可靠的临床用α-淀粉酶抑制剂方面的当代挑战和潜在途径,总结了该领域的最新研究。

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Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, and anti-diabetic evaluation.噻唑烷-2,4-二酮杂合物作为双α-淀粉酶和α-葡萄糖苷酶抑制剂:设计、合成及抗糖尿病评价
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