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
收藏
页码：2195 / 2208
页数：14
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