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
-
Drug Design for Neglected Disease in Brazil
Mini-Reviews in Medicinal Chemistry Critical Illness in Obstetric Patients: Introduction and Epidemiology
Current Women`s Health Reviews Food Allergy
Current Pharmaceutical Design MRI of the Small and Large Bowel
Current Medical Imaging Protease Inhibitors as Promising Weapons against COVID-19: Focus on Repurposing of Drugs used to Treat HIV and HCV Infections
Current Topics in Medicinal Chemistry Development of Electrochromic Devices
Recent Patents on Nanotechnology Novel Pharmacologic Approaches to the Management of Sepsis: Targeting the Host Inflammatory Response
Recent Patents on Inflammation & Allergy Drug Discovery IoT Solutions for Smart Management of Hospital Buildings: A General Review towards COVID-19, Future Pandemics, and Infectious Diseases
Current Signal Transduction Therapy Molecular Modelling Approaches to the Design of Acetylcholinesterase Inhibitors: New Challenges for the Treatment of Alzheimers Disease
Current Pharmaceutical Design REVIEWER ACKNOWLEDGEMENT
Current Pharmacogenomics and Personalized Medicine High Resolution Magic Angle Spinning NMR for Analyzing Small Molecules Attached to Solid Support
Combinatorial Chemistry & High Throughput Screening Preface
Recent Advances in Drug Delivery and Formulation Natural Agents Modulating ACE-2: A Review of Compounds with Potential against SARS-CoV-2 Infections
Current Pharmaceutical Design Mesenchymal Stromal Cells and their EVs as Potential Leads for SARSCoV2 Treatment
Current Stem Cell Research & Therapy Toward Small-Molecule Inhibition of Protein–Protein Interactions: General Aspects and Recent Progress in Targeting Costimulatory and Coinhibitory (Immune Checkpoint) Interactions
Current Topics in Medicinal Chemistry Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 2. Structural Analogues and Derivatives
Current Drug Targets Synthesis and Urease Inhibitory Properties of Some New N4-Substituted 5-Nitroisatin-3-thiosemicarbazones
Letters in Drug Design & Discovery Chitosan Nanoparticles: A Therapeutic Carrier for Delivery of DNA, siRNA and CpG-ODNs
Nanoscience & Nanotechnology-Asia Ligand-Receptor Communication and Drug Design
Current Protein & Peptide Science Functional Polymeric Nano/Microparticles for Surface Adsorption and Delivery of Protein and DNA Vaccines
Current Drug Delivery