Abstract
There has been an increasing interest in compounds that modulate potassium ion channels (K+-channels) since they can be developed as important therapeutic agents against ischemic heart diseases. Of the diverse family of K+- channels, the voltage-gated potassium channel Kv1.3 constitutes an attractive target for the selective suppression of effector memory T cells in autoimmune diseases. For the development of antiarrythmic drugs, the blockade of the rapidly activating delayed rectifier (IKr) and slowly activating delayed rectifier (IKs) potassium currents has been specifically studied. Since the discovery of IKs-channel, its blockers have been particularly more studied. In this communication, we present QSAR studies on a few series of Kv1.3-channel blockers and a series of IKs-channel blockers in order to provide some guidelines to the drug development.
Keywords: Quantitative structure-activity relationship study, potassium channel blockers, Kv1.3-channel blockers, IKschannel blockers, khellinone analogs, chromanols
Medicinal Chemistry
Title: A Quantitative Structure-Activity Relationship Study on Some Series of Potassium Channel Blockers
Volume: 5 Issue: 1
Author(s): V. S.A. Kumar Satuluri, Jyostna Seelam and S. P. Gupta
Affiliation:
Keywords: Quantitative structure-activity relationship study, potassium channel blockers, Kv1.3-channel blockers, IKschannel blockers, khellinone analogs, chromanols
Abstract: There has been an increasing interest in compounds that modulate potassium ion channels (K+-channels) since they can be developed as important therapeutic agents against ischemic heart diseases. Of the diverse family of K+- channels, the voltage-gated potassium channel Kv1.3 constitutes an attractive target for the selective suppression of effector memory T cells in autoimmune diseases. For the development of antiarrythmic drugs, the blockade of the rapidly activating delayed rectifier (IKr) and slowly activating delayed rectifier (IKs) potassium currents has been specifically studied. Since the discovery of IKs-channel, its blockers have been particularly more studied. In this communication, we present QSAR studies on a few series of Kv1.3-channel blockers and a series of IKs-channel blockers in order to provide some guidelines to the drug development.
Export Options
About this article
Cite this article as:
Kumar Satuluri S.A. V., Seelam Jyostna and Gupta P. S., A Quantitative Structure-Activity Relationship Study on Some Series of Potassium Channel Blockers, Medicinal Chemistry 2009; 5 (1) . https://dx.doi.org/10.2174/157340609787049244
DOI https://dx.doi.org/10.2174/157340609787049244 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
-
Fc-Independent Phagocytosis: Implications for Intravenous IgG Therapy in Immune Thrombocytopenia
Cardiovascular & Hematological Disorders-Drug Targets Insights into the Relationship Between Hypertension and Albuminuria
Current Hypertension Reviews Cardiovascular Disease Risk Among the Poor and Homeless – What We Know So Far
Current Cardiology Reviews Current Algorithms for the Diagnosis of wide QRS Complex Tachycardias
Current Cardiology Reviews ATP-Binding Cassette Transporters A1 and G1, HDL Metabolism, Cholesterol Efflux, and Inflammation: Important Targets for the Treatment of Atherosclerosis
Current Drug Targets Opportunities and Challenges in Nano-structure Mediated Drug Delivery: Where Do We Stand?
Current Nanomedicine Epidemiology of Gout: Perspectives from the Past
Current Rheumatology Reviews Aging and Oral Health: Effects in Hard and Soft Tissues
Current Pharmaceutical Design Homocysteine in Neurology: From Endothelium to Neurodegeneration
Current Nutrition & Food Science Neutrophil Function in Severe Sepsis
Endocrine, Metabolic & Immune Disorders - Drug Targets The Use of SIFT-MS to Investigate Headspace Aldehydes as Markers of Lipid Peroxidation
Current Analytical Chemistry Hypertensive Treatment and the Metabolic Syndrome
Current Hypertension Reviews Vasorelaxant and Antihypertensive Effects of <i>Mentha pulegium</i> L. in Rats: An In vitro and In vivo Approach
Endocrine, Metabolic & Immune Disorders - Drug Targets CRP Pro-inflammatory Signalling in Atherosclerosis: Myth or Reality?
Current Signal Transduction Therapy Tianeptine: A Novel Atypical Antidepressant that May Provide New Insights into the Biomolecular Basis of Depression
Recent Patents on CNS Drug Discovery (Discontinued) Structure and Expression of Different Serum Amyloid A (SAA) Variants and their Concentration-Dependent Functions During Host Insults
Current Medicinal Chemistry Common Features of the Metabolic Syndrome and Nonalcoholic Fatty Liver Disease
Reviews on Recent Clinical Trials Hybrid Molecules Development: A Versatile Landscape for the Control of Antifungal Drug Resistance: A Review
Mini-Reviews in Medicinal Chemistry Inflammatory Systemic Biomarkers in Setting Acute Coronary Syndromes - Effects of the Diurnal Variation
Current Drug Targets Mobile Phone Based Biomedical Imaging Technology: A Newly Emerging Area
Recent Patents on Biomedical Engineering (Discontinued)