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

IF 3.2 4区 医学 Q3 CHEMISTRY, MEDICINAL Future medicinal chemistry Pub Date : 2025-02-01 Epub Date: 2025-01-21 DOI:10.1080/17568919.2025.2453421
Rahul Singh, Jayant Sindhu, Devender Singh, Parvin Kumar
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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 in vitro, in silico and in vivo 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.

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α-淀粉酶抑制剂开发中的关键分子支架。
2型糖尿病病例的不断增加,加上当前降糖药的不良副作用,促使了餐后血糖水平管理的创新方法的发展。α-淀粉酶是一种内酰胺酶,负责分解膳食淀粉中的α-1,4-糖苷键,产生低聚糖。随后,α-葡萄糖苷酶将这些低聚糖降解为单糖,这些单糖被吸收到血液中并为人体所利用。α-淀粉酶抑制剂降低了碳水化合物的消化率,同时延迟了葡萄糖的吸收,导致餐后血糖水平下降,因此,抑制α-淀粉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。本文综述了最近发现的潜在α-淀粉酶抑制剂的治疗前景,重点介绍了它们的体外、硅和体内研究概况。最后,我们总结了该领域的最新研究,阐述了在寻找安全可靠的α-淀粉酶抑制剂用于临床应用方面面临的挑战和未来的潜在途径。
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来源期刊
Future medicinal chemistry
Future medicinal chemistry CHEMISTRY, MEDICINAL-
CiteScore
5.80
自引率
2.40%
发文量
118
审稿时长
4-8 weeks
期刊介绍: Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.
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