Open Access
Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors
Aida Iraji
1, 2
,
Diba Shareghi Brojeni
3
,
Somayeh Mojtabavi
4
,
Mohammad Ali Faramarzi
4
,
Tahmineh Akbarzadeh
3, 5
,
Mina Saeedi
5, 6
5
Publication type: Journal Article
Publication date: 2022-05-23
scimago Q1
wos Q1
SJR: 0.874
CiteScore: 6.7
Impact factor: 3.9
ISSN: 20452322
PubMed ID:
35606520
Multidisciplinary
Abstract
In this work, a novel series of cyanoacetohydrazide linked to 1,2,3-triazoles (9a–n) were designed and synthesized to be evaluated for their anti-α-glucosidase activity, focusing on the fact that α-glucosidase inhibitors have played a significant role in the management of type 2 diabetes mellitus. All synthesized compounds except 9a exhibited excellent inhibitory potential, with IC50 values ranging from 1.00 ± 0.01 to 271.17 ± 0.30 μM when compared to the standard drug acarbose (IC50 = 754.1 ± 0.5 μM). The kinetic binding study indicated that the most active derivatives 9b (IC50 = 1.50 ± 0.01 μM) and 9e (IC50 = 1.00 ± 0.01 μM) behaved as the uncompetitive inhibitors of α-glucosidase with Ki = 0.43 and 0.24 μM, respectively. Moreover, fluorescence measurements were conducted to show conformational changes of the enzyme after binding of the most potent inhibitor (9e). Calculation of standard enthalpy (ΔHm°) and entropy (ΔSm°) values confirmed the construction of hydrophobic interactions between 9e and the enzyme. Also, docking studies indicated desired interactions with important residues of the enzyme which rationalized the in vitro results.
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40
Total citations:
40
Citations from 2024:
24
(60%)
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GOST
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Iraji A. et al. Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors // Scientific Reports. 2022. Vol. 12. No. 1. 8647
GOST all authors (up to 50)
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Iraji A., Shareghi Brojeni D., Mojtabavi S., Faramarzi M. A., Akbarzadeh T., Saeedi M. Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors // Scientific Reports. 2022. Vol. 12. No. 1. 8647
Cite this
RIS
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TY - JOUR
DO - 10.1038/s41598-022-11771-y
UR - https://doi.org/10.1038/s41598-022-11771-y
TI - Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors
T2 - Scientific Reports
AU - Iraji, Aida
AU - Shareghi Brojeni, Diba
AU - Mojtabavi, Somayeh
AU - Faramarzi, Mohammad Ali
AU - Akbarzadeh, Tahmineh
AU - Saeedi, Mina
PY - 2022
DA - 2022/05/23
PB - Springer Nature
IS - 1
VL - 12
PMID - 35606520
SN - 2045-2322
ER -
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BibTex (up to 50 authors)
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@article{2022_Iraji,
author = {Aida Iraji and Diba Shareghi Brojeni and Somayeh Mojtabavi and Mohammad Ali Faramarzi and Tahmineh Akbarzadeh and Mina Saeedi},
title = {Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors},
journal = {Scientific Reports},
year = {2022},
volume = {12},
publisher = {Springer Nature},
month = {may},
url = {https://doi.org/10.1038/s41598-022-11771-y},
number = {1},
pages = {8647},
doi = {10.1038/s41598-022-11771-y}
}