Abstract
A series of N-aroylated isatins 1-15 was synthesized and evaluated for their antiglycation activity. All compounds showed a varying degree of glycation inhibitory activity with IC50 values between 18.01 ± 0.05-693.7 ± 3.0 μM, when compared with the standard (aminoguanidine) having an IC50 = 268.7 ± 12.4 μM. Compound 1 was found to be the most active member of this series with an IC50 = 18.01 ± 0.05 μM. Compound 10 showed an IC50 = 72.5 ± 0.09 μM, whereas compound 7 has an IC50 = 80.18 ± 0.07 μM. Compounds 3, 9, and 13 showed IC50 values 170.2 ± 0.62, 117.91 ± 2.9, 171.3 ± 0.79 μM, respectively. Rest of the compounds along with parent isatin were found to be inactive. The structures of all the synthetic compounds were deduced by spectroscopic analysis.
Keywords: Isatin, N-Aroylation, Antiglycation, Lead molecules
Letters in Drug Design & Discovery
Title: N-Aroylated Isatins: Antiglycation Activity
Volume: 7 Issue: 3
Author(s): Khalid Mohammed Khan, Uzma Rasool Mughal, Ambreen Khan, Farzana Naz, Shahnaz Perveen and M. Iqbal Choudhary
Affiliation:
Keywords: Isatin, N-Aroylation, Antiglycation, Lead molecules
Abstract: A series of N-aroylated isatins 1-15 was synthesized and evaluated for their antiglycation activity. All compounds showed a varying degree of glycation inhibitory activity with IC50 values between 18.01 ± 0.05-693.7 ± 3.0 μM, when compared with the standard (aminoguanidine) having an IC50 = 268.7 ± 12.4 μM. Compound 1 was found to be the most active member of this series with an IC50 = 18.01 ± 0.05 μM. Compound 10 showed an IC50 = 72.5 ± 0.09 μM, whereas compound 7 has an IC50 = 80.18 ± 0.07 μM. Compounds 3, 9, and 13 showed IC50 values 170.2 ± 0.62, 117.91 ± 2.9, 171.3 ± 0.79 μM, respectively. Rest of the compounds along with parent isatin were found to be inactive. The structures of all the synthetic compounds were deduced by spectroscopic analysis.
Export Options
About this article
Cite this article as:
Khan Mohammed Khalid, Mughal Rasool Uzma, Khan Ambreen, Naz Farzana, Perveen Shahnaz and Choudhary Iqbal M., N-Aroylated Isatins: Antiglycation Activity, Letters in Drug Design & Discovery 2010; 7 (3) . https://dx.doi.org/10.2174/157018010790596597
DOI https://dx.doi.org/10.2174/157018010790596597 |
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
-
Insect Peptides – Perspectives in Human Diseases Treatment
Current Medicinal Chemistry Single Amino Acid Repeats Connect Viruses to Neurodegeneration
Current Drug Discovery Technologies Directions for Enhancement of the Therapeutic Efficacy of Mesenchymal Stem Cells in Different Neurodegenerative and Cardiovascular Diseases: Current Status and Future Perspectives
Current Stem Cell Research & Therapy Anti-Inflammatory Therapy for Alzheimer’s Disease from Epidemiological Fact to New Mechanisms of Action
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Editorial [Hot Topic: Regulation of Glutamate Synthesis Via Inhibition of Glutamate Carboxypeptidase II (GCPII): An Effective Method to Treat Central and Peripheral Nervous System Disorders (Guest Editors: Guido Cavaletti and Barbara Slusher)]
Current Medicinal Chemistry Etiopathogenesis, Classical Immunotherapy and Innovative Nanotherapeutics for Inflammatory Neurological Disorders
Current Nanoscience The Role of microRNAs in the Development of Type 2 Diabetes Complications
Current Pharmaceutical Design Dysregulation of RNA Mediated Gene Expression in Motor Neuron Diseases
CNS & Neurological Disorders - Drug Targets Emerging Potential of Natural Products as an Alternative Strategy to Pharmacological Agents Used Against Metabolic Disorders
Current Drug Metabolism Coumarin Compounds in Medicinal Chemistry: Some Important Examples from the Last Years
Current Topics in Medicinal Chemistry Subject Index To Volume 3
Current Alzheimer Research Role of Oxidative Stress in Development of Cardiovascular Complications in Diabetes Mellitus
Current Vascular Pharmacology Oxidative Imbalance and Anxiety Disorders
Current Neuropharmacology On the Pathogenesis and Neuroprotective Treatment of Parkinson Disease: What have we Learned from the Genetic Forms of this Disease?
Current Medicinal Chemistry Cross-Talk Between NO Synthase Isoforms in Neuro-Inflammation: Possible Implications in HIV-Associated Neurocognitive Disorders
Current Medicinal Chemistry Phytochemicals as PI3K/ Akt/ mTOR Inhibitors and Their Role in Breast Cancer Treatment
Recent Patents on Anti-Cancer Drug Discovery Cell-based Treatment of Cerebral Palsy: Still a Long Way Ahead
Current Stem Cell Research & Therapy Role of Nitrosative Stress and Poly(ADP-ribose) Polymerase Activation in Diabetic Vascular Dysfunction
Current Vascular Pharmacology Pharmacological Interventions on Asymmetric Dimethylarginine, a Clinical Marker of Vascular Disease
Current Medicinal Chemistry Are Gap Junction Channels a Therapeutic Target and if so What Properties are Best Exploited?
Current Drug Targets