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

被引：19

作者：

Moghimi, Setareh ^{[1
]}

Toolabi, Mahsa ^{[2
]}

Salarinejad, Somayeh ^{[3
]}

Firoozpour, Loghman ^{[1
]}

Ebrahimi, Seyed Esmaeil Sadat ^{[3
]}

Safari, Fatemeh ^{[4
]}

Mojtabavi, Somayeh ^{[5
]}

Faramarzi, Mohammad Ali ^{[5
]}

Foroumadi, Alireza ^{[1
,3
]}

机构：

[1] Univ Tehran Med Sci, Inst Pharmaceut Sci TIPS, Drug Design & Dev Res Ctr, Tehran, Iran

[2] Ahvaz Jundishapur Univ Med Sci, Sch Pharm, Dept Med Chem, Ahvaz, Iran

[3] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran

[4] Univ Guilan, Fac Sci, Dept Biol, Rasht, Iran

[5] Univ Tehran Med Sci, Fac Pharm, Dept Pharmaceut Biotechnol, Tehran, Iran

来源：

BIOORGANIC CHEMISTRY | 2020年 / 102卷

基金：

美国国家科学基金会;

关键词：

Pyridazine; Glucosidase inhibitor; Lawesson's reagent; Antidiabetic drug; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; POTENT; DRUG; BIOISOSTERISM; DERIVATIVES;

D O I：

10.1016/j.bioorg.2020.104071

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 alpha-glucosidase enzyme. In-vitro alpha-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited alpha-glucosidase with the IC50 value of 70.1 mu M. 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.

引用

页数：9

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