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

Author:

Talab Faiz1,Zainab 2,Alam Aftab1,Ali Mumtaz1,Rehman Najeeb Ur3,Ullah Saeed3,Halim Sobia Ahsan3,Islam Mohammad Shahidul4,Khan Ajmal3,Latif Abdul1,Ayaz Muhammad1,Al-Ghafri Ahmed3,Al-Harrasi Ahmed3,Ahmad Manzoor1ORCID

Affiliation:

1. Department of Chemistry, University of Malakand, PO Box 18800, Dir Lower, Khyber Pakhtunkhwa, Pakistan

2. College of Chemistry & Materials Science, Hebei Normal University, Shijiazhuang, 050024, China

3. Natural & Medical Sciences Research Center, University of Nizwa, Nizwa, 616, Oman

4. Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh, 11451, Saudi Arabia

Abstract

Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of α-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Methods: Polyhydroquinoline derivatives (1–17) were synthesized and tested for in vitro α-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 μM, compared with the standard drug, acarbose. The binding mechanism of these derivatives with α-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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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