Abstract
Background: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for the risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them.
Methods: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity. The binding modes of potent compounds in the active site of α-glucosidase enzyme were also explored through molecular docking studies.
Results and Conclusion: Among the reported triazoles, compounds 3-9, 11, and 13 (IC50 = 6.0 ± 0.03 to 19.8 ± 0.28 µM) were found to be several fold more active than the standard drug acarbose (IC50 = 840 ± 1.73 µM). Compound 5 (IC50 = 6.0 ± 0.03 µM) was the most potent AGIs in the series, about 77- fold more active than acarbose. Therefore, dibenzoazepine linked-triazoles described here can serve as leads for further studies as new non-sugar AGIs.
Keywords: Acetophenones, diabetes, dibenzoazepine, molecular docking, triazoles, α-glucosidase.
Medicinal Chemistry
Title:In vitro α-Glucosidase Inhibition by Non-sugar based Triazoles of Dibenzoazepine, their Structure-Activity Relationship, and Molecular Docking
Volume: 13 Issue: 7
Author(s): Maria A. Khan*, Kulsoom Javaid, Abdul Wadood, Alam Jamal, Farhana Batool, Saba Fazal-ur-Rehman, Fatima Z. Basha and Muhammad I. Choudhary
Affiliation:
- H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270,Pakistan
Keywords: Acetophenones, diabetes, dibenzoazepine, molecular docking, triazoles, α-glucosidase.
Abstract: Background: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for the risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them.
Methods: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity. The binding modes of potent compounds in the active site of α-glucosidase enzyme were also explored through molecular docking studies.
Results and Conclusion: Among the reported triazoles, compounds 3-9, 11, and 13 (IC50 = 6.0 ± 0.03 to 19.8 ± 0.28 µM) were found to be several fold more active than the standard drug acarbose (IC50 = 840 ± 1.73 µM). Compound 5 (IC50 = 6.0 ± 0.03 µM) was the most potent AGIs in the series, about 77- fold more active than acarbose. Therefore, dibenzoazepine linked-triazoles described here can serve as leads for further studies as new non-sugar AGIs.
Export Options
About this article
Cite this article as:
Khan A. Maria *, Javaid Kulsoom , Wadood Abdul , Jamal Alam , Batool Farhana , Fazal-ur-Rehman Saba , Basha Z. Fatima and Choudhary I. Muhammad, In vitro α-Glucosidase Inhibition by Non-sugar based Triazoles of Dibenzoazepine, their Structure-Activity Relationship, and Molecular Docking, Medicinal Chemistry 2017; 13 (7) . https://dx.doi.org/10.2174/1573406413666170726142949
DOI https://dx.doi.org/10.2174/1573406413666170726142949 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Disturbance of Inorganic Phosphate Metabolism in Diabetes Mellitus: Its Impact on the Development of Diabetic Late Complications
Current Diabetes Reviews Mechanisms of Endothelial Dysfunction: Clinical Significance and Preventive Non-Pharmacological Therapeutic Strategies
Current Pharmaceutical Design Neuroinflammation and Immunity: A New Pharmacological Target in Depression
CNS & Neurological Disorders - Drug Targets Identification of Neuronal Nitric Oxide Synthase (nNOS) in Human Penis: a Potential Role of Reduced Neuronally-derived Nitric Oxide in Erectile Dysfunction
Current Pharmaceutical Biotechnology Evolving Strategies in Manipulating VEGF/VEGFR Signaling for the Promotion of Angiogenesis in Ischemic Muscle
Current Pharmaceutical Design Alkaptonuria, Ochronosis and Ochronotic Arthropathy in Mainland France and the Reunion Island. A Report of Clinical and Molecular Findings in 29 Patients
Current Rheumatology Reviews Embryonic Stem Cells: Overcoming the Immunological Barriers to Cell Replacement Therapy
Current Stem Cell Research & Therapy Interleukin-25: Key Regulator of Inflammatory and Autoimmune Diseases
Current Pharmaceutical Design Metabolomics and the Diagnosis of Human Diseases -A Guide to the Markers and Pathophysiological Pathways Affected
Current Medicinal Chemistry Pharmacogenomics in Psychiatry: Implications for Practice
Recent Patents on Biotechnology Does Phosphodiesterase 11A (PDE11A) Hold Promise as a Future Therapeutic Target?
Current Pharmaceutical Design Editorial (Hot Topic: Achieving Current Goals in Prevention and Treatment of Vascular Disease: An Update)
Current Pharmaceutical Design HIV-Therapy Associated Lipodystrophy: Experimental and Clinical Evidence for the Pathogenesis and Treatment
Endocrine, Metabolic & Immune Disorders - Drug Targets Lipid Disorders in Pregnancy
Current Pharmaceutical Design Autophagy as a Molecular Target of Flavonoids Underlying their Protective Effects in Human Disease
Current Medicinal Chemistry Screening for Silent Coronary Artery Disease in Diabetics- or Not?
Current Diabetes Reviews Independent Relationship between Serum Osteocalcin and Uric Acid in a Cohort of Apparently Healthy Obese Subjects
Endocrine, Metabolic & Immune Disorders - Drug Targets Renal Ischemia: How Commonly Does it Cause Renal Failure?
Current Hypertension Reviews Disorders of Sex Development: A Review
Current Women`s Health Reviews A Review on the Effects of New Anti-Diabetic Drugs on Platelet Function
Endocrine, Metabolic & Immune Disorders - Drug Targets