Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

被引：32

作者：

Noori, Milad ^{[1
]}

Davoodi, Ali ^{[2
]}

Iraji, Aida ^{[3
,4
]}

Dastyafteh, Navid ^{[1
]}

Khalili, Minoo ^{[1
]}

Asadi, Mehdi ^{[2
]}

Khanaposhtani, Maryam Mohammadi ^{[5
]}

Mojtabavi, Somayeh ^{[6
,7
]}

Dianatpour, Mehdi ^{[3
]}

Faramarzi, Mohammad Ali ^{[6
,7
]}

Larijani, Bagher ^{[1
]}

Amanlou, Massoud ^{[2
]}

Mahdavi, Mohammad ^{[1
]}

机构：

[1] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, Iran

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

[3] Shiraz Univ Med Sci, Stem Cells Technol Res Ctr, Shiraz, Iran

[4] Shiraz Univ Med Sci, Cent Res Lab, Shiraz, Iran

[5] Babol Univ Med Sci, Cellular & Mol Biol Res Ctr, Hlth Res Inst, Babol, Iran

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

[7] Univ Tehran Med Sci, Biotechnol Res Ctr, Tehran, Iran

来源：

SCIENTIFIC REPORTS | 2022年 / 12卷 / 01期

关键词：

NATURAL-PRODUCTS;

D O I：

10.1038/s41598-022-18455-7

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their alpha-glucosidase inhibitory potential. All compounds in the series except 9q showed a significant alpha-glucosidase inhibition with IC50 values in the range of 3.2 +/- 0.3-185.0 +/- 0.3 mu M, as compared to the standard drug acarbose (IC50 = 750.0 +/- 5.0 mu M). A kinetic study indicated that compound 9d as the most potent derivative against alpha-glucosidase was a competitive type inhibitor. Furthermore, the molecular docking study revealed the effective binding interactions of 9d with the active site of the alpha-glucosidase enzyme. The results indicate that the designed compounds have the potential to be further studied as new anti-diabetic agents.

引用

页数：13

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