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香豆素与 2-苯基苯并咪唑衍生物作为有效的α-葡萄糖苷酶抑制剂的联系。

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors.

机构信息

Department of Chemistry, College of Basic Sciences, Yadegar-e-Imam Khomeini (RAH) Shahre Rey Branch, Islamic Azad University, Tehran, Iran.

Department of Biology, College of Basic Sciences, Yadegar-e-Imam Khomeini (RAH) Shahre Rey Branch, Islamic Azad University, Tehran, Iran.

出版信息

Sci Rep. 2024 Mar 28;14(1):7408. doi: 10.1038/s41598-024-57673-z.

DOI:10.1038/s41598-024-57673-z
PMID:38548784
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10978946/
Abstract

α-Glucosidase inhibitors have emerged as crucial agents in the management of type 2 diabetes mellitus. In the present study, a new series of coumarin-linked 2-phenylbenzimidazole derivatives 5a-m was designed, synthesized, and evaluated as anti-α-glucosidase agents. Among these derivatives, compound 5k (IC = 10.8 µM) exhibited a significant inhibitory activity in comparison to the positive control acarbose (IC = 750.0 µM). Through kinetic analysis, it was revealed that compound 5k exhibited a competitive inhibition pattern against α-glucosidase. To gain insights into the interactions between the title compounds and α-glucosidase molecular docking was employed. The obtained results highlighted crucial interactions that contribute to the inhibitory activities of the compounds against α-glucosidase. These derivatives show immense potential as promising starting points for developing novel α-glucosidase inhibitors.

摘要

α-葡萄糖苷酶抑制剂已成为 2 型糖尿病治疗的重要药物。在本研究中，设计、合成了一系列新型香豆素连接的 2-苯基苯并咪唑衍生物 5a-m，并评估其作为抗α-葡萄糖苷酶试剂的活性。在这些衍生物中，化合物 5k（IC = 10.8 μM）的抑制活性明显优于阳性对照阿卡波糖（IC = 750.0 μM）。通过动力学分析，发现化合物 5k 对α-葡萄糖苷酶表现出竞争性抑制模式。为了深入了解这些化合物与α-葡萄糖苷酶的相互作用，采用分子对接技术进行了研究。获得的结果突出了化合物与α-葡萄糖苷酶相互作用的关键，这些相互作用有助于化合物抑制α-葡萄糖苷酶的活性。这些衍生物具有很大的潜力，可作为开发新型α-葡萄糖苷酶抑制剂的起始点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/b1ca6f85b7ca/41598_2024_57673_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/f1b524e14a40/41598_2024_57673_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/c514b7ff9e9a/41598_2024_57673_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/b679ddf95a66/41598_2024_57673_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/dc3f53e2f9ba/41598_2024_57673_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/eeb998eb3ccf/41598_2024_57673_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/861e9b4ebc3e/41598_2024_57673_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/b1ca6f85b7ca/41598_2024_57673_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/f1b524e14a40/41598_2024_57673_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/c514b7ff9e9a/41598_2024_57673_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/b679ddf95a66/41598_2024_57673_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/dc3f53e2f9ba/41598_2024_57673_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/eeb998eb3ccf/41598_2024_57673_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/861e9b4ebc3e/41598_2024_57673_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1d7/10978946/b1ca6f85b7ca/41598_2024_57673_Fig6_HTML.jpg

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