Abstract
1,3,4-oxadiazole, a privileged structure, endows its derivatives with broad and potent biological functions, especially in antiviral activities, including anti-HIV, anti-HCV, anti-HBV, anti-HSV activities, etc. Molecular modeling and pharmacokinetic studies have demonstrated that the introduction of 1,3,4-oxadiazole ring to the inhibitors can change their polarity, flexibility as well as metabolic stability, and 1,3,4-oxadiazole scaffold can also act as acceptors of hydrogen bonds formation, which make it possible to be used as a isosteric substituent for amide or ester groups.
This review focuses on the recent advances in the synthesis of 1,3,4-oxadiazole ring and mainly the discovery, biological activities investigations and structural modifications of several distinct classes of 1,3,4-oxadiazoles as potent antiviral agents. In addition, the binding models of some representative 1,3,4-oxadiazoles were also discussed, which provide rational explanation for their interesting antiviral activities, and also pave the way for further optimization of 1,3,4- oxadiazole based antiviral agents.
Keywords: 1, 3, 4-Oxadiazole, privileged structure, solid-phase synthesis, antiviral activity, structural modification, molecule modeling, scaffold, Microwave-Assisted, NNRTIs, alkenyldiarylmethanes, Protease Inhibitors, Integrase Inhibitors
Mini-Reviews in Medicinal Chemistry
Title: 1,3,4-Oxadiazole: A Privileged Structure in Antiviral Agents
Volume: 11 Issue: 13
Author(s): Z. Li, P. Zhan and X. Liu
Affiliation:
Keywords: 1, 3, 4-Oxadiazole, privileged structure, solid-phase synthesis, antiviral activity, structural modification, molecule modeling, scaffold, Microwave-Assisted, NNRTIs, alkenyldiarylmethanes, Protease Inhibitors, Integrase Inhibitors
Abstract: 1,3,4-oxadiazole, a privileged structure, endows its derivatives with broad and potent biological functions, especially in antiviral activities, including anti-HIV, anti-HCV, anti-HBV, anti-HSV activities, etc. Molecular modeling and pharmacokinetic studies have demonstrated that the introduction of 1,3,4-oxadiazole ring to the inhibitors can change their polarity, flexibility as well as metabolic stability, and 1,3,4-oxadiazole scaffold can also act as acceptors of hydrogen bonds formation, which make it possible to be used as a isosteric substituent for amide or ester groups.
This review focuses on the recent advances in the synthesis of 1,3,4-oxadiazole ring and mainly the discovery, biological activities investigations and structural modifications of several distinct classes of 1,3,4-oxadiazoles as potent antiviral agents. In addition, the binding models of some representative 1,3,4-oxadiazoles were also discussed, which provide rational explanation for their interesting antiviral activities, and also pave the way for further optimization of 1,3,4- oxadiazole based antiviral agents.
Export Options
About this article
Cite this article as:
Li Z., Zhan P. and Liu X., 1,3,4-Oxadiazole: A Privileged Structure in Antiviral Agents, Mini-Reviews in Medicinal Chemistry 2011; 11 (13) . https://dx.doi.org/10.2174/138955711797655407
DOI https://dx.doi.org/10.2174/138955711797655407 |
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
Drugs and mitochondria
Mitochondria play a central role in the life and death of cells. They are not merely the center for energy metabolism but are also the headquarters for different catabolic and anabolic processes, calcium fluxes, and various signaling pathways. Mitochondria maintain homeostasis in the cell by interacting with reactive oxygen-nitrogen species ...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
-
Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas
Medicinal Chemistry Multiresolution Denoising for Optical Coherence Tomography: A Review and Evaluation
Current Medical Imaging Skirmishing Disconcerting Covid-19 by Drug Reassigning
Applied Drug Research, Clinical Trials and Regulatory Affairs Structure-based Virtual Screening, Molecular Docking, Molecular Dynamics Simulation, and Metabolic Reactivity Studies of Quinazoline Derivatives for their Anti-EGFR Activity Against Tumor Angiogenesis
Current Medicinal Chemistry Is Testosterone the “Fountain of Youth” for Aging Men?
Endocrine, Metabolic & Immune Disorders - Drug Targets Utilization of Telehealth in Kenya During COVID-19
Coronaviruses Natural Products as Farnesoid X Receptor (FXR) Agonists: Their Interactions with FXR Ligand Binding Region
Mini-Reviews in Organic Chemistry The Bioisosteric Concept Applied to Cannabinoid Ligands
Current Medicinal Chemistry The Topology of Molecule and Its Lipophilicity
Current Computer-Aided Drug Design Pharmacokinetic Properties and In Silico ADME Modeling in Drug Discovery
Medicinal Chemistry Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles
Letters in Drug Design & Discovery Lipid-based Nanoparticles (LNP) Structures used for Drug Delivery and Targeting: Clinical Trials and Patents
Nanoscience & Nanotechnology-Asia Drug Repurposing in the Development of Anticancer Agents
Current Medicinal Chemistry Identification of Functional Peptides from Natural and Synthetic Products on Their Anticancer Activities by Tumor Targeting
Current Medicinal Chemistry Recent Progress in the Research of Small Molecule HIV-1 RNase H Inhibitors
Current Medicinal Chemistry Anti-cancer Potential of Phyto-alkaloids: A Prospective Review
Current Cancer Therapy Reviews Oxidative Status in Multiple Sclerosis and Off-Targets of Antioxidants: The Case of Edaravone
Current Medicinal Chemistry Innovative Approaches for Controlling Clinically Relevant Biofilms: Current Trends and Future Prospects
Current Topics in Medicinal Chemistry New Developments in Inhaled Antibiotics for the Treatment of Pseudomonas aeruginosa
Current Pharmaceutical Design Radioligands for the Angiotensin II Subtype 1 (AT1) Receptor
Current Topics in Medicinal Chemistry