Abstract
Schiff bases of isatin 1-20 were synthesized and tested for their antiglycation potential. Compound 6 showed 77% inhibition with an IC50= 177.2 ± 0.4 μM, which is an excellent antiglycation activity, if compared with standard aminoguanidine having 85.69% inhibition with an IC50 value 268.7 ± 12.4 μM. Compound 3 showed 71.3% inhibition with an IC = 675 ± 0.12 μ/M, which is moderately active antiglycation agent. Although compounds 1, 2, 5, 7-15, and 17- 19 demonstrated over 50% inhibition in preliminary screening, but found inactive when further evaluated for their IC values. However, compounds 4, 16, 20, and parent isatin showed less than 50% inhibition and considered to be completely inactive. The structures of all the synthesized compounds were determined by spectroscopic analysis, including UV, IR, mass and 1H-NMR spectrometry. All compounds gave satisfactory elemental analysis.
Keywords: Synthesis, Isatin, Schiff bases, Antiglycation, Lead molecules
Letters in Drug Design & Discovery
Title: Schiff Bases of Istain: Antiglycation Activity
Volume: 6 Issue: 5
Author(s): Khalid Mohammed Khan, Uzma Rasool Mughal, Nida Ambreen, Ambreen Khan, Shahnaz Perveen and Muhammad Iqbal Choudhary
Affiliation:
Keywords: Synthesis, Isatin, Schiff bases, Antiglycation, Lead molecules
Abstract: Schiff bases of isatin 1-20 were synthesized and tested for their antiglycation potential. Compound 6 showed 77% inhibition with an IC50= 177.2 ± 0.4 μM, which is an excellent antiglycation activity, if compared with standard aminoguanidine having 85.69% inhibition with an IC50 value 268.7 ± 12.4 μM. Compound 3 showed 71.3% inhibition with an IC = 675 ± 0.12 μ/M, which is moderately active antiglycation agent. Although compounds 1, 2, 5, 7-15, and 17- 19 demonstrated over 50% inhibition in preliminary screening, but found inactive when further evaluated for their IC values. However, compounds 4, 16, 20, and parent isatin showed less than 50% inhibition and considered to be completely inactive. The structures of all the synthesized compounds were determined by spectroscopic analysis, including UV, IR, mass and 1H-NMR spectrometry. All compounds gave satisfactory elemental analysis.
Export Options
About this article
Cite this article as:
Khan Mohammed Khalid, Mughal Rasool Uzma, Ambreen Nida, Khan Ambreen, Perveen Shahnaz and Choudhary Iqbal Muhammad, Schiff Bases of Istain: Antiglycation Activity, Letters in Drug Design & Discovery 2009; 6 (5) . https://dx.doi.org/10.2174/1570180810906050358
DOI https://dx.doi.org/10.2174/1570180810906050358 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Redox Status in Periodontal and Systemic Inflammatory Conditions Including Associated Neoplasias: Antioxidants as Adjunctive Therapy?
Infectious Disorders - Drug Targets Motor Neuron Disease and Acquired Axonal Neuropathy Association in HIV Infection: Case Report and Update
Current HIV Research Towards Newer Molecular Targets for Chronic Diabetic Complications
Current Vascular Pharmacology Is there a Rational Approach for Increasing Drug Specificity? Considerations on CNS Target Choice and Validation
Recent Patents on CNS Drug Discovery (Discontinued) Patent Annotations
Recent Patents on Cardiovascular Drug Discovery Non-Ceruloplasmin Copper Distinguishes A Distinct Subtype of Alzheimer’s Disease: A Study of EEG-Derived Brain Activity
Current Alzheimer Research Aldose Reductase, Still a Compelling Target for Diabetic Neuropathy
Current Drug Targets Molecular Mechanism Aspect of ER Stress in Alzheimer's Disease: Current Approaches and Future Strategies
Current Drug Targets Editorial (Hot Topic: Regenerative Medicine in Neurological Diseases)
Recent Patents on Regenerative Medicine IGF-I Signaling in Response to Hyperglycemia and the Development of Diabetic Complications
Current Diabetes Reviews Endocannabinoid System in Neurological Disorders
Recent Patents on CNS Drug Discovery (Discontinued) A Molecular Approach on the Protective Effects of Mangiferin Against Diabetes and Diabetes-related Complications
Current Diabetes Reviews Extranuclear Localization of SIRT1 and PGC-1α: An Insight into Possible Roles in Diseases Associated with Mitochondrial Dysfunction
Current Molecular Medicine Non-Celiac Gluten Sensitivity Triggers Gut Dysbiosis, Neuroinflammation, Gut-Brain Axis Dysfunction, and Vulnerability for Dementia
CNS & Neurological Disorders - Drug Targets Editorial [Hot Topic:Role of Neural Stem Cells in Neurodegenerative Diseases:From the Molecule and Cell to the Clinic (Guest Editor: Oscar Gonzalez-Perez)]
Current Signal Transduction Therapy New Hope for the Diagnosis and Therapy of Alzheimers Disease
Protein & Peptide Letters Recent Studies of Aldose Reductase Enzyme Inhibition for Diabetic Complications
Current Medicinal Chemistry Prevention and treatment of atherosclerosis with flaxseed -derived compound secoisolariciresinol diglucoside
Current Pharmaceutical Design Review on Patents for Potent Anticoagulant Antithrombin-Heparin Covalent Complexes that Control Thrombosis In Vivo
Recent Patents on Biomedical Engineering (Discontinued) Advanced Glycation End Products as Environmental Risk Factors for the Development of Type 1 Diabetes
Current Drug Targets