Abstract
Synthesis of a series of urea and thiourea derivatives of glycine and proline conjugated to 2,3-dichlorophenyl piperazine has been reported. The structures were confirmed by physical and spectroscopical measurements followed by characterization of antiglycation activity. All synthesized compounds were able to inhibit protein glycation, particularly halogen containing derivatives without preference of oxygen or sulphur at the urea function. The best analogues are nearly 20 fold (< 5 µM) more potent than the reference standard, rutin (41.9 µM).
Keywords: Amino acids, piperazine, conjugation, urea/thiourea, antiglycation.
Protein & Peptide Letters
Title:Synthesis and SAR Studies of Urea and Thiourea Derivatives of Gly/Pro Conjugated to Piperazine Analogue as Potential AGE Inhibitors
Volume: 20 Issue: 8
Author(s): Doddahindaiah M. Suyoga Vardhan, Chavalmane S. Shantharam, Ramesh Suhas, Malavalli B. Sridhara and D. Channe Gowda
Affiliation:
Keywords: Amino acids, piperazine, conjugation, urea/thiourea, antiglycation.
Abstract: Synthesis of a series of urea and thiourea derivatives of glycine and proline conjugated to 2,3-dichlorophenyl piperazine has been reported. The structures were confirmed by physical and spectroscopical measurements followed by characterization of antiglycation activity. All synthesized compounds were able to inhibit protein glycation, particularly halogen containing derivatives without preference of oxygen or sulphur at the urea function. The best analogues are nearly 20 fold (< 5 µM) more potent than the reference standard, rutin (41.9 µM).
Export Options
About this article
Cite this article as:
Vardhan M. Suyoga Doddahindaiah, Shantharam S. Chavalmane, Suhas Ramesh, Sridhara B. Malavalli and Gowda Channe D., Synthesis and SAR Studies of Urea and Thiourea Derivatives of Gly/Pro Conjugated to Piperazine Analogue as Potential AGE Inhibitors, Protein & Peptide Letters 2013; 20 (8) . https://dx.doi.org/10.2174/0929866511320080005
DOI https://dx.doi.org/10.2174/0929866511320080005 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
- 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
-
Common Genetic Variants of the Mitochondrial Trafficking System and Mitochondrial Uncoupling Proteins Affect the Development of Two Slowly Developing Demyelinating Disorders, Leukoaraiosis and Multiple Sclerosis
Current Medicinal Chemistry Cannabinoids and Neuroprotection in Motor-Related Disorders
CNS & Neurological Disorders - Drug Targets Meet Our Associate Editor
Current Molecular Medicine Inhibitory Effects of β-Cyclodextrin and Trehalose on Nanofibril and AGE Formation During Glycation of Human Serum Albumin
Protein & Peptide Letters Cellular, Molecular and Non-Pharmacological Therapeutic Advances for the Treatment of Parkinson's Disease: Separating Hope from Hype
Current Gene Therapy Prospects for Kinase Activity Modulators in the Treatment of Diabetes and Diabetic Complications
Current Topics in Medicinal Chemistry One-pot Synthesis of Dihydropyrano[2,3-c]chromenes via a Three-component Reaction in Aqueous Media
Combinatorial Chemistry & High Throughput Screening The Panomics Approach in Neurodegenerative Disorders
Current Medicinal Chemistry Recent Multi-target Approaches on the Development of Anti- Alzheimer's Agents Integrating Metal Chelation Activity
Current Medicinal Chemistry Editorial [Hot Topic: Vascular Complications of Diabetes (Executive Editor: Olga I. Stenina)]
Current Pharmaceutical Design CD147: A Novel Modulator of Inflammatory and Immune Disorders
Current Medicinal Chemistry The Small Heat Shock Protein HspB8: Role in Nervous System Physiology and Pathology
CNS & Neurological Disorders - Drug Targets The Role of Microglial Cell Subsets in Alzheimers Disease
Current Alzheimer Research MicroRNAs: Biomarkers for Cardiovascular Disease in Patients with Diabetes Mellitus
Current Topics in Medicinal Chemistry Progressive Brain Damage and Alterations in Dendritic Arborization after Collagenase-Induced Intracerebral Hemorrhage in Rats
Current Neurovascular Research VEGF Signaling Regulates Cofilin and the Arp2/3-complex within the Axonal Growth Cone
Current Neurovascular Research Linking Alzheimer’s Disease and Type 2 Diabetes Mellitus via Aberrant Insulin Signaling and Inflammation
CNS & Neurological Disorders - Drug Targets From the Table to the Bedside: Can Food-Derived Sulforaphane be used as a Novel Agent to Treat Leukemia?
Current Cancer Drug Targets Carcinogenesis and Diabetic Wound Healing: Evidences of Parallelism
Current Diabetes Reviews The Complex Biology of FOXO
Current Drug Targets