Abstract
In addition to their antihistamine effects, H1-receptor antagonists possess pharmacological properties that are not uniformly distributed among this class of drugs, such as anti-inflammatory, anti-allergic and antiplatelet activities. In this paper, Cyclizine (1-benzhydryl-4-methyl-piperazine, I), bromodiphenhydramine (2-[(4-bromophenyl)- phenylmethoxy]-N, N-dimethylethanamine, II) and some of their new piperazine and ethanolamine derivatives (III-VIII) inducing changes in substitution of phenyl and amine moieties were synthesized and their acute and chronic antiinflammatory effects were evaluated by standard pharmacological tests. The results showed that substitution of phenyl by tolyl, anisol and cumene groups in piperazine family could remarkably decrease acute inflammation in these new drugs. Also, substitution of dimethylamine by morpholine group could not decrease this inflammation in new synthesized ethanolamine family. But the results from the cotton pellet-induced granuloma formation in rats showed that none of drugs (I-VIII) were effective to reduce the chronic inflammation.
Keywords: Acute and chronic anti-inflammation effects, Cyclizine, Bromo diphenhydramine, H1-receptor antagonist, Piperazine and ethanolamine derivatives.
Mini-Reviews in Medicinal Chemistry
Title:Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H1-antihistaminic drugs
Volume: 12 Issue: 12
Author(s): Abbas Ahmadi, Mohsen Khalili, Ali Nafarie, Arash Yazdani and Babak Nahri-Niknafs
Affiliation:
Keywords: Acute and chronic anti-inflammation effects, Cyclizine, Bromo diphenhydramine, H1-receptor antagonist, Piperazine and ethanolamine derivatives.
Abstract: In addition to their antihistamine effects, H1-receptor antagonists possess pharmacological properties that are not uniformly distributed among this class of drugs, such as anti-inflammatory, anti-allergic and antiplatelet activities. In this paper, Cyclizine (1-benzhydryl-4-methyl-piperazine, I), bromodiphenhydramine (2-[(4-bromophenyl)- phenylmethoxy]-N, N-dimethylethanamine, II) and some of their new piperazine and ethanolamine derivatives (III-VIII) inducing changes in substitution of phenyl and amine moieties were synthesized and their acute and chronic antiinflammatory effects were evaluated by standard pharmacological tests. The results showed that substitution of phenyl by tolyl, anisol and cumene groups in piperazine family could remarkably decrease acute inflammation in these new drugs. Also, substitution of dimethylamine by morpholine group could not decrease this inflammation in new synthesized ethanolamine family. But the results from the cotton pellet-induced granuloma formation in rats showed that none of drugs (I-VIII) were effective to reduce the chronic inflammation.
Export Options
About this article
Cite this article as:
Ahmadi Abbas, Khalili Mohsen, Nafarie Ali, Yazdani Arash and Nahri-Niknafs Babak, Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H1-antihistaminic drugs, Mini-Reviews in Medicinal Chemistry 2012; 12 (12) . https://dx.doi.org/10.2174/138955712802762013
DOI https://dx.doi.org/10.2174/138955712802762013 |
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
-
Design, Synthesis and Biological Evaluation of Benzimidazole-pyridine- Piperidine Hybrids as a New Class of Potent Antimicrobial Agents
Letters in Drug Design & Discovery Development of Environment-Friendly Insecticides Based on Enantioselectivity: Bifenthrin as a Case
Current Protein & Peptide Science Immune-Neuroendocrine Interactions Involving Thymus and Pineal Gland in Stem Cell Therapy of Age-Related Diseases
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Metabolism of Δ³-Carene by Human Cytochrome P450 Enzymes: Identification and Characterization of Two New Metabolites
Current Drug Metabolism <i>Cannabis Sativa</i> L. Flower and Bud Extracts Inhibited <i>In vitro</i> Cholinesterases and β-Secretase Enzymes Activities: Possible Mechanisms of Cannabis Use in Alzheimer Disease
Endocrine, Metabolic & Immune Disorders - Drug Targets Mining for Protein Kinase Substrates: Integration of Biochemistry, Genetics and Proteomics
Current Proteomics 7-prenyloxi-6-methoxycoumarin from Polygala sabulosa A.W. Bennett Regulates p38 MAPK and NF-kB Pathways Inhibiting the Inflammation Induced by Carrageenan in the Mouse Model of Pleurisy
Inflammation & Allergy - Drug Targets (Discontinued) Bicyclol: A Novel Drug for Treating Chronic Viral Hepatitis B and C
Medicinal Chemistry The Role of Transesophageal Echocardiography in the Intraoperative Period
Current Cardiology Reviews The Detection of Pb<sup>2+</sup> Using Glutathione Capped Mn Doped ZnS QDs
Current Analytical Chemistry The Influence of Natural Substrates and Inhibitors on the Nucleotide- Dependent Excision Activity of HIV-1 Reverse Transcriptase in the Infected Cell
Current Pharmaceutical Design Synthesis and in vitro Evaluation of the Anticancer Potential of New Aminoalkanol Derivatives of Xanthone
Anti-Cancer Agents in Medicinal Chemistry Sonochemical Hot-spot Assisted One-pot Synthesis of 4-arylmethylidene - 2-phenyl-4H-oxazol-5-ones Using Nano-MgO as an Efficient Catalyst
Letters in Organic Chemistry Synthesis and Anticancer Activity of Phthalimido and Naphthalimido Substituted Dihydropyrimidone Conjugates
Letters in Drug Design & Discovery Surgical Approach to Ulcerative Colitis: When is the Best Timing after Medical Treatment?
Current Drug Targets A Review on Phytochemistry and Pharmacology of Medicinal as well as Poisonous Mushrooms
Mini-Reviews in Medicinal Chemistry Circulating Meteorin-like Levels in Patients with Type 2 Diabetes Mellitus: A Meta-Analysis
Current Pharmaceutical Design Natural Antioxidants in Wheat Sprout Extracts
Current Organic Chemistry Electrochemical Behavior and Square-Wave Stripping Voltammetric Determination of Roflumilast in Pharmaceutical Dosage Forms
Combinatorial Chemistry & High Throughput Screening Hybrid Pharmacophore Design and Synthesis of Naphthalimide– Benzimidazole Conjugates as Potential Anticancer Agents
Letters in Drug Design & Discovery