Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches

被引：15

作者：

Talab, Faiz ^{[1
]}

Zainab, Aftab ^{[2
]}

Alam, Aftab ^{[1
,2
]}

Ali, Mumtaz ^{[1
]}

Rehman, Najeeb Ur ^{[1
,3
]}

Ullah, Saeed ^{[3
]}

Halim, Sobia Ahsan ^{[3
]}

Islam, Mohammad Shahidul ^{[4
]}

Khan, Ajmal ^{[3
]}

Latif, Abdul ^{[1
]}

Ayaz, Muhammad ^{[1
]}

Al-Ghafri, Ahmed ^{[3
]}

Al-Harrasi, Ahmed ^{[3
]}

Ahmad, Manzoor ^{[1
]}

机构：

[1] Univ Malakand, Dept Chem, POB 18800, Totakan, Khyber Pakhtunk, Pakistan

[2] Hebei Normal Univ, Coll Chem & Mat Sci, Shijiazhuang 050024, Peoples R China

[3] Univ Nizwa, Nat & Med Sci Res Ctr, Nizwa 616, Oman

[4] King Saud Univ, Coll Sci, Dept Chem, POB 2455, Riyadh 11451, Saudi Arabia

来源：

FUTURE MEDICINAL CHEMISTRY | 2023年 / 15卷 / 23期

关键词：

molecular docking; NMR spectroscopy; polyhydroquinoline; structure-activity relationship; alpha-glucosidase; ALPHA-GLUCOSIDASE; MOLECULAR DOCKING; CATALYST; PATHWAY;

D O I：

10.4155/fmc-2023-0232

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of alpha-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Methods: Polyhydroquinoline derivatives (1-17) were synthesized and tested for in vitro alpha-glucosidase inhibitory activity. Results: All the synthesized compounds exhibited excellent to good inhibitory activity, having IC50 values from 1.23 +/- 0.03 to 73.85 +/- 0.61 mu M, compared with the standard drug, acarbose. The binding mechanism of these derivatives with alpha-glucosidase was deduced by docking studies and indicated that a slight variation in the orientation of compounds, affects their binding capability. Conclusion: In order to find new antidiabetic drugs, this study has discovered prospective lead candidates.

引用

页码：2195 / 2208

页数：14

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