Abstract
Given their many physiological functions, KATP channels represent promising drug targets. Sulfonylureas like glibenclamide block KATP channels; they are used in the therapy of type 2 diabetes. Openers of KATP channels (KCOs) e.g. relax smooth muscle and induce hypotension. KCOs are chemically heterogeneous and include as different classes as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines and pyridyl nitrates. Examples for new chemical entities more recently developed as KCOs include cyclobutenediones, dihydropyridine related structures, and tertiary carbinols. Structure-activity relationships of the main chemical classes of KCOs are discussed.
Keywords: KATP channel openers (KCOs), structure-activity relationships, benzopyrans, cyanoguanidines, thioformamides, diazoxide, cyclobutenediones, dihydropyridine related structures, tertiary carbinols
Current Topics in Medicinal Chemistry
Title: Structure-Activity Relationships of KATP Channel Openers
Volume: 6 Issue: 10
Author(s): Raimund Mannhold
Affiliation:
Keywords: KATP channel openers (KCOs), structure-activity relationships, benzopyrans, cyanoguanidines, thioformamides, diazoxide, cyclobutenediones, dihydropyridine related structures, tertiary carbinols
Abstract: Given their many physiological functions, KATP channels represent promising drug targets. Sulfonylureas like glibenclamide block KATP channels; they are used in the therapy of type 2 diabetes. Openers of KATP channels (KCOs) e.g. relax smooth muscle and induce hypotension. KCOs are chemically heterogeneous and include as different classes as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines and pyridyl nitrates. Examples for new chemical entities more recently developed as KCOs include cyclobutenediones, dihydropyridine related structures, and tertiary carbinols. Structure-activity relationships of the main chemical classes of KCOs are discussed.
Export Options
About this article
Cite this article as:
Mannhold Raimund, Structure-Activity Relationships of KATP Channel Openers, Current Topics in Medicinal Chemistry 2006; 6 (10) . https://dx.doi.org/10.2174/156802606777323647
DOI https://dx.doi.org/10.2174/156802606777323647 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
Rho Kinase Inhibitors and Novel Ocular Drug Delivery Systems- A Revolutionary Step Towards the Treatment of Glaucoma
Current Drug Delivery Neuroprotective Effects of Drug-Induced Therapeutic Hypothermia in Central Nervous System Diseases
Current Drug Targets Endocannabinoids and their Involvement in the Neurovascular System
Current Neurovascular Research Anabolic Androgenic Steroids Abuse and Liver Toxicity
Mini-Reviews in Medicinal Chemistry Vasopressin & Oxytocin in Control of the Cardiovascular System: An Updated Review
Current Neuropharmacology Usefulness of Home Blood Pressure in the Diagnosis and Control of Hypertension in Primary Care
Current Hypertension Reviews Atrial Tachycardias Occurring Late After Open Heart Surgery
Current Cardiology Reviews Pharmacological Treatment of Hypertension in Pregnancy
Current Pharmaceutical Design Simultaneous Determination of Cytochrome P450 Oxidation Capacity in Humans: A Review on the Phenotyping Cocktail Approach
Current Pharmaceutical Biotechnology The Reno-Protective Effect of the Dual Blockade of the Renin Angiotensin System (RAS)
Current Pharmaceutical Design Ambulatory Blood Pressure and Diabetes: Targeting Nondipping
Current Diabetes Reviews The Cardiorenal Syndrome: Pathophysiologic Crosstalk, Outcomes, and Treatment Targets
Cardiovascular & Hematological Disorders-Drug Targets Schizophrenia: A Systematic Review of the Disease State, Current Therapeutics and their Molecular Mechanisms of Action
Current Medicinal Chemistry Management of Acute Aluminum Phosphide Poisoning: Has Anything Changed?
Drug Metabolism Letters Immunotherapy of Melanoma
Current Molecular Pharmacology CGRP-Receptor Antagonism in Migraine Treatment
CNS & Neurological Disorders - Drug Targets Medication-Induced Nephrotoxicity in Older Patients
Current Drug Metabolism Polyphenols: A Nutraceutical Approach Against Diseases
Recent Patents on Food, Nutrition & Agriculture Naturally Occurring and Related Synthetic Cannabinoids and their Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Thrombolytic Treatment of Cardiac Myxoma-Induced Ischemic Stroke: A Review
Current Drug Safety