Abstract
Phthalimide and hydrazine pharmacophores have been demonstrated to be inhibitors of cyclooxygenases (COX) and lipoxygenases (LOX) and to possess a marked analgesic and anti-inflammatory activity. A new group of hybrid analogs of phthalimide and hydrazine (2-(arylmethylideneamino) isoindolines), possessing a variety of substituents (OMe, OH, NO2, Cl, and F) at different positions of the aryl ring, were synthesized and their analgesic and anti-inflammatory effects were evaluated. In vivo screening showed that all the analogs possessed analgesic and anti-inflammatory activity and compounds 10g, 10h and 10e were the most potent as analgesic and compounds 10b, 10c and 10i were the most potent as anti-inflammatory agents.
Keywords: Analgesic, anti-inflammatory, hydrazone, isoindoline, phthalimide.
Current Pharmaceutical Design
Title:Design and Synthesis of 2-(Arylmethylideneamino) Isoindolines as New Potential Analgesic and Anti-Inflammatory Agents: A Molecular Hybridization Approach
Volume: 22 Issue: 37
Author(s): Maryam Iman, Hamed Shafaroodi, Asghar Davood, Masoud Abedini, Pouyan Pishva, Mehrnoush Taherkhani, Ahmad Reza Dehpour and Abbas Shafiee
Affiliation:
Keywords: Analgesic, anti-inflammatory, hydrazone, isoindoline, phthalimide.
Abstract: Phthalimide and hydrazine pharmacophores have been demonstrated to be inhibitors of cyclooxygenases (COX) and lipoxygenases (LOX) and to possess a marked analgesic and anti-inflammatory activity. A new group of hybrid analogs of phthalimide and hydrazine (2-(arylmethylideneamino) isoindolines), possessing a variety of substituents (OMe, OH, NO2, Cl, and F) at different positions of the aryl ring, were synthesized and their analgesic and anti-inflammatory effects were evaluated. In vivo screening showed that all the analogs possessed analgesic and anti-inflammatory activity and compounds 10g, 10h and 10e were the most potent as analgesic and compounds 10b, 10c and 10i were the most potent as anti-inflammatory agents.
Export Options
About this article
Cite this article as:
Iman Maryam, Shafaroodi Hamed, Davood Asghar, Abedini Masoud, Pishva Pouyan, Taherkhani Mehrnoush, Dehpour Reza Ahmad and Shafiee Abbas, Design and Synthesis of 2-(Arylmethylideneamino) Isoindolines as New Potential Analgesic and Anti-Inflammatory Agents: A Molecular Hybridization Approach, Current Pharmaceutical Design 2016; 22 (37) . https://dx.doi.org/10.2174/1381612822666160701072127
DOI https://dx.doi.org/10.2174/1381612822666160701072127 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Development and Validation of a Highly Sensitive HPLC Method for Determination of Paclitaxel in Pharmaceutical Dosage forms and Biological Samples
Current Pharmaceutical Analysis Roles of Natural Compounds from Medicinal Plants in Cancer Treatment: Structure and Mode of Action at Molecular Level
Medicinal Chemistry Evaluation of Herbal Medicines: Value Addition to Traditional Medicines Through Metabolism, Pharmacokinetic and Safety Studies
Current Drug Metabolism Metabolism of Flavonoids in Human: A Comprehensive Review
Current Drug Metabolism Flavonoids: The Innocuous Agents Offering Protection against Alzheimer’s Disease Through Modulation of Proinflammatory and Apoptotic Pathways
Current Topics in Medicinal Chemistry High Performance Liquid Chromatographic Approaches to Mass Spectrometry Based Metabolomics
Current Metabolomics Inhibition of Transcription Factors by Plant-Derived Compounds and their Implications in Inflammation and Cancer
Current Pharmaceutical Design Biophysical Screening for Identifying Pharmacological Chaperones and Inhibitors Against Conformational and Infectious Diseases
Current Drug Targets QSAR Models for Proteins of Parasitic Organisms, Plants and Human Guests: Theory, Applications, Legal Protection, Taxes, and Regulatory Issues
Current Proteomics In Vitro Selection of a Single-Stranded DNA Molecular Recognition Element for the Pesticide Malathion
Combinatorial Chemistry & High Throughput Screening The Synthesis, Structural Modification and Mode of Anticancer Action of Evodiamine: A Review
Recent Patents on Anti-Cancer Drug Discovery Peptide Self-assembly: From Toxins to Amyloid Fibrils and Nanotubes
Current Topics in Medicinal Chemistry Steroid Regulation of Drug-Metabolizing Cytochromes P450
Current Drug Metabolism Design, Synthesis and Evaluation of Novel 2-piperidinyl Quinoline Chalcones/ Amines as Potential Antidepressant Agents
Letters in Drug Design & Discovery Molecular Pathology and Molecular Markers of Ductal Carcinoma in-situ
Current Cancer Therapy Reviews Fructooligosaccharides of Edible Alliums: Occurrence, Chemistry and Health Benefits
Current Nutrition & Food Science Nanocrystals as Effective Delivery Systems of Poorly Water-soluble Natural Molecules
Current Medicinal Chemistry An Overview of Neolignans of the Genus Piper L.: Isolation Methods and Biological Activities
Mini-Reviews in Medicinal Chemistry Multifaceted Synthesis, Properties and Applications of Polyurethanes and its Composites
Current Organic Chemistry Chitosan Nanoparticles for Melanoma Cancer Treatment by Photodynamic Therapy and Electrochemotherapy Using Aminolevulinic Acid Derivatives
Current Medicinal Chemistry