Design and synthesis of novel pyridazine N-aryl acetamides: In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies.,Bioorganic Chemistry

当前位置： X-MOL 学术 › Bioorgan. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Design and synthesis of novel pyridazine N-aryl acetamides: In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-07-06 , DOI: 10.1016/j.bioorg.2020.104071
Setareh Moghimi ₁ , Mahsa Toolabi ₂ , Somayeh Salarinejad ₃ , Loghman Firoozpour ₁ , Seyed Esmaeil Sadat Ebrahimi ₃ , Fatemeh Safari ₄ , Somayeh Mojtabavi ₅ , Mohammad Ali Faramarzi ₅ , Alireza Foroumadi ₆

Affiliation

We herein applied the four step-synthetic route to prepare the pyridazine core attached to the various N-aryl acetamides. By this approach, a new series of pyridazine-based compounds were synthesized, characterized and evaluated for their activities against α-glucosidase enzyme. In-vitro α-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited α-glucosidase with the IC₅₀ value of 70.1 µM. The most potent compounds showed no cytotoxicity against HDF cell line. Molecular docking and kinetic studies were performed to determine the modes of interaction and inhibition, respectively.

中文翻译：

新型哒嗪N-芳基乙酰胺的设计和合成：α-葡萄糖苷酶抑制，对接和动力学研究的体外评估。

我们在此应用了四步合成路线来制备与各种N-芳基乙酰胺连接的哒嗪核心。通过这种方法，合成了一系列新的基于哒嗪的化合物，表征并评估了它们对α-葡萄糖苷酶的活性。在-体外α葡糖苷酶测定法确定，12个的化合物比阿卡波糖更有效。化合物7a抑制α-葡萄糖苷酶，IC ₅₀值为70.1 µM。最有效的化合物对HDF细胞系无细胞毒性。进行了分子对接和动力学研究，以确定相互作用和抑制的模式。

更新日期：2020-07-17

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11