Abstract
Pyridazinone derivatives and their related analoges were introduced for gastric antiulcer and antisecretory activities. Selected compounds were applied to ulcer models and showed their antiulcer and anti secretary activities. Some pyridazinone compounds are recently reported as H3R antagonists. Some amine analogs of pyridazinones, pyridazinone– phenethylamines and 4,5-fused pyridazinones showed histamine H3R antagonist activity with significant affinity for rat and human H3R. These pyridazinone analogs also showed excellent selectivity and metabolic stability, with adequate pharmacokinetics.
Keywords: Antiulcer, antagonist, antisecretory, histamine, H3 receptor, pyridazinones.
Mini-Reviews in Medicinal Chemistry
Title:A Mini Review on Biological Activities of Pyridazinone Derivatives as Antiulcer, Antisecretory, antihistamine and Particularly Against Histamine H3R
Volume: 14 Issue: 13
Author(s): Mohammad Asif
Affiliation:
Keywords: Antiulcer, antagonist, antisecretory, histamine, H3 receptor, pyridazinones.
Abstract: Pyridazinone derivatives and their related analoges were introduced for gastric antiulcer and antisecretory activities. Selected compounds were applied to ulcer models and showed their antiulcer and anti secretary activities. Some pyridazinone compounds are recently reported as H3R antagonists. Some amine analogs of pyridazinones, pyridazinone– phenethylamines and 4,5-fused pyridazinones showed histamine H3R antagonist activity with significant affinity for rat and human H3R. These pyridazinone analogs also showed excellent selectivity and metabolic stability, with adequate pharmacokinetics.
Export Options
About this article
Cite this article as:
Asif Mohammad, A Mini Review on Biological Activities of Pyridazinone Derivatives as Antiulcer, Antisecretory, antihistamine and Particularly Against Histamine H3R, Mini-Reviews in Medicinal Chemistry 2014; 14 (13) . https://dx.doi.org/10.2174/1389557514666141127143133
DOI https://dx.doi.org/10.2174/1389557514666141127143133 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
-
Are the Antioxidant Properties of Carvedilol Important for the Protection of Cardiac Mitochondria?
Current Vascular Pharmacology Amniotic Fluid Embolism: Moving Diagnosis Through the Time. From the Mechanical Pulmonary Vascular Occlusion Until An Immuno - Inflammatory Pathogenesis?
Current Pharmaceutical Biotechnology An Update on Peptide Drugs for Voltage-Gated Calcium Channels
Recent Patents on CNS Drug Discovery (Discontinued) Recent Development in Applications of Important Biopolymer Chitosan in Biomedicine, Pharmaceuticals and Personal Care Products
Current Tissue Engineering (Discontinued) Advanced Therapies For End-Stage Heart Failure
Current Cardiology Reviews Impact of Clozapine, N-Desmethylclozapine and Chlorpromazine on Thromboxane Production in Vitro
Medicinal Chemistry Enhanced Anticancer Activity and Apoptosis Effect of Bioactive Compound Quercetin Extracted from <i>Ocimum sanctum</i> Leaves
Current Nanomedicine Rationalizing the Study of Plants for the Treatment of Oral Pain
Current Chemical Biology Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets?
Current Molecular Pharmacology Do RAS Inhibitors Protect the Brain from Cerebral Ischemic Injury?
Current Hypertension Reviews A Clinician’s Guide to Monoamine Oxidase Inhibitors
Current Psychiatry Reviews Mechanisms of Cardiovascular Changes in an Experimental Model of Syndrome X and Pharmacological Intervention on the Renin-Angiotensin- System
Current Vascular Pharmacology Pharmacological Neuroprotection after Perinatal Hypoxic-Ischemic Brain Injury
Current Neuropharmacology Selective Serotonin Re-Uptake Inhibitors for the Treatment of Depression in Coronary Artery Disease and Chronic Heart Failure: Evidence for Pleiotropic Effects
Cardiovascular & Hematological Agents in Medicinal Chemistry Metal Complexes, their Cellular Targets and Potential for Cancer Therapy
Current Pharmaceutical Design Neuroprotective Effects of Intravenous Anesthetics: A New Critical Perspective
Current Pharmaceutical Design Pharmacological Approaches in the Treatment of Atrial Fibrillation
Current Medicinal Chemistry Antidotes for Acute Cyanide Poisoning
Current Pharmaceutical Biotechnology Oral Antidiabetic Agents: Anti-Atherosclerotic Properties Beyond Glucose Lowering?
Current Pharmaceutical Design Standardization Using Analytical Techniques (UV, NMR, FTIR, HPLC, Mass) and Pharmacognostic Evaluation of the Roots of <i>Selinum vaginatum</i>: A Rare Himalayan Plant of the Rohtang Region
Current Biotechnology