Abstract
Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and –NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.
Keywords: N-substituted TZDs, antidiabetic, anticancer, anti-inflammatory, aldose reductase activity, alkonic acid.
Mini-Reviews in Medicinal Chemistry
Title:Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions
Volume: 19 Issue: 4
Author(s): Rakesh Gupta, Hardik Joshi and C.S. Ramaa*
Affiliation:
- Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi-Mumbai,India
Keywords: N-substituted TZDs, antidiabetic, anticancer, anti-inflammatory, aldose reductase activity, alkonic acid.
Abstract: Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and –NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.
Export Options
About this article
Cite this article as:
Gupta Rakesh , Joshi Hardik and Ramaa C.S. *, Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions, Mini-Reviews in Medicinal Chemistry 2019; 19 (4) . https://dx.doi.org/10.2174/1389557518666171129163426
DOI https://dx.doi.org/10.2174/1389557518666171129163426 |
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
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
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
New Therapeutics to Modulate Mitochondrial Function in Neurodegenerative Disorders
Current Pharmaceutical Design Prevention and Treatment of Diabetic Retinopathy: Evidence from Large, Randomized Trials. The Emerging Role of Fenofibrate
Reviews on Recent Clinical Trials Lewy Bodies: A Spectator or Salient Killer?
CNS & Neurological Disorders - Drug Targets Autologous Mesenchymal Stem Cell Therapy in Progressive Multiple Sclerosis: An Open Label Study
Current Stem Cell Research & Therapy Docking of Natural Products against Neurodegenerative Diseases: General Concepts
Combinatorial Chemistry & High Throughput Screening Review of 5-HT4R Ligands: State of Art and Clinical Applications
Current Topics in Medicinal Chemistry The Contribution of Proteinase-Activated Receptors to Intracellular Signaling, Transcellular Transport and Autophagy in Alzheimer´s Disease
Current Alzheimer Research FKBP Ligands as Novel Therapeutics for Neurological Disorders
Mini-Reviews in Medicinal Chemistry Do Adenosine Receptors Offer New Therapeutic Options for Diabetic Nephropathy?
Current Vascular Pharmacology Neurobiology of Depression and Novel Antidepressant Drug Targets
Current Pharmaceutical Design Prevalence, Incidence, Risk and Protective Factors of Amnestic Mild Cognitive Impairment in the Elderly in Shanghai
Current Alzheimer Research Antioxidants in Treating Pathologies Involving Oxidative Damage: An Update on Medicinal Chemistry and Biological Activity of Stobadine and Related Pyridoindoles
Current Medicinal Chemistry Oxidative Stress and Skeletal Muscle Dysfunction with Aging
Current Aging Science Emerging Targets and Latest Proteomics Based Therapeutic Approaches in Neurodegenerative Diseases
Current Protein & Peptide Science Nutraceutical Approach to Peripheral Neuropathies: Evidence from Clinical Trials
Current Drug Metabolism Relationship Between Body Mass Index and Reproduction
Current Women`s Health Reviews Endothelial Progenitor Cells and Vascular Biology in Diabetes Mellitus: Current Knowledge and Future Perspectives
Current Diabetes Reviews Surrogate Outcomes for Progression in the Initial Stages of Diabetic Retinopathy
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Current Therapies and Emerging Targets for the Treatment of Diabetes
Current Pharmaceutical Design Neurodegeneration in the Brain Tumor Microenvironment: Glutamate in the Limelight
Current Neuropharmacology