Abstract
A series of novel 1,2,4-triazole derivatives has been designed and synthesized. All of the new compounds were evaluated for their anti-HIV activities in MT-4 cells. Three of them showed moderate activities against wild-type HIV-1 with an EC50 ranging from 17.4 μM to 4.87 μM. Among the active compounds, 3-((4-(3,4-dimethoxybenzylideneamino)- 5-(furan-2-yl)-4H-1,2,4-triazol-3-ylthio)methyl)benzonitrile (4d) was identified as the promising compound (EC50 = 17.4 μM, SI =13). However, no compound displayed inhibitory activity against HIV-2.
Keywords: HIV-1, AIDS, NNRTIs, Triazoles, Synthesis, Anti-HIV-1 activity, NNRTIs, LC Autosampler Device, heterocyclic scaffold, Nexus 470FT-IR
Letters in Drug Design & Discovery
Title:Synthesis and Anti-HIV Evaluation of Novel 1,2,4-triazole Derivatives as Potential Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors
Volume: 10 Issue: 1
Author(s): Zhenyu Li, Yuan Cao, Peng Zhan, Christophe Pannecouque, Jan Balzarini, Erik De Clercq and Xinyong Liu
Affiliation:
Keywords: HIV-1, AIDS, NNRTIs, Triazoles, Synthesis, Anti-HIV-1 activity, NNRTIs, LC Autosampler Device, heterocyclic scaffold, Nexus 470FT-IR
Abstract: A series of novel 1,2,4-triazole derivatives has been designed and synthesized. All of the new compounds were evaluated for their anti-HIV activities in MT-4 cells. Three of them showed moderate activities against wild-type HIV-1 with an EC50 ranging from 17.4 μM to 4.87 μM. Among the active compounds, 3-((4-(3,4-dimethoxybenzylideneamino)- 5-(furan-2-yl)-4H-1,2,4-triazol-3-ylthio)methyl)benzonitrile (4d) was identified as the promising compound (EC50 = 17.4 μM, SI =13). However, no compound displayed inhibitory activity against HIV-2.
Export Options
About this article
Cite this article as:
Li Zhenyu, Cao Yuan, Zhan Peng, Pannecouque Christophe, Balzarini Jan, De Clercq Erik and Liu Xinyong, Synthesis and Anti-HIV Evaluation of Novel 1,2,4-triazole Derivatives as Potential Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors, Letters in Drug Design & Discovery 2013; 10 (1) . https://dx.doi.org/10.2174/1570180811309010027
DOI https://dx.doi.org/10.2174/1570180811309010027 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Recent Developments of C-Aryl Glucoside SGLT2 Inhibitors
Current Medicinal Chemistry Patent Selections:
Recent Patents on Anti-Infective Drug Discovery Progress on the Biological Activities of Helicid and its Derivatives
Current Organic Chemistry Novel Proline Derivatives for Treating COVID-19
Current Medicinal Chemistry Influence of SGLT2 Inhibitors in Remodeling, Substrate and Ion Metabolism of Myocardium to Prevent Cardiovascular Risks: Recent Work and Advancement
Current Molecular Pharmacology Computational Screening and Design for Compounds that Disrupt Protein-protein Interactions
Current Topics in Medicinal Chemistry Anti-Cancer Potential of Some Commonly Used Drugs
Current Pharmaceutical Design An Approach to Synthesis of 3-Aryl-2-Oxazolidinones and In Situ`Click` Assembly of 1,2,3-Triazole Oxazolidinones
Letters in Organic Chemistry Pharmacogenetics of Antihypertensive Therapies: Can this be Applied in the Clinic?
Current Pharmacogenomics and Personalized Medicine Recent Progress in Rational Drug Design of Neuraminidase Inhibitors
Current Medicinal Chemistry High-Throughput Screening by Nuclear Magnetic Resonance (HTS by NMR) for the Identification of PPIs Antagonists
Current Topics in Medicinal Chemistry Fate of Ionic Liquids in Soils and Sediments
Current Organic Chemistry Physiology and Pharmacology of the Vanilloid Receptor
Current Neuropharmacology Anti-Diabetic Drugs GLP-1 Agonists and DPP-4 Inhibitors may Represent Potential Therapeutic Approaches for COVID-19
Endocrine, Metabolic & Immune Disorders - Drug Targets Anti-MRSA (Multidrug Resistant Staphylococcus aureus) Activity of 3-Substituted Coumarins
Letters in Drug Design & Discovery Experimental Approaches Towards Allergic Asthma Therapy-Murine Asthma Models
Recent Patents on Inflammation & Allergy Drug Discovery Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry Structural Biology and Drug Discovery
Current Pharmaceutical Design Translocator Protein Ligands as Promising Therapeutic Tools for Anxiety Disorders
Current Medicinal Chemistry Structure-Activity Relationships for Serotonin Transporter and Dopamine Receptor Selectivity
Medicinal Chemistry