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
-
COVID-19 and Brain Aging: What are the Implications of Immunosenescence?
Current Aging Science GluN2B/N-methyl-D-aspartate Receptor Antagonists: Advances in Design, Synthesis, and Pharmacological Evaluation Studies
CNS & Neurological Disorders - Drug Targets Design, Synthesis and Biological Evaluation of 4, 6-Coumarin Derivatives as Anti- Cancer and Apoptosis-Inducing Agents
Anti-Cancer Agents in Medicinal Chemistry 2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line
Mini-Reviews in Medicinal Chemistry Invited Editorial: MERS-CoV An Emerging Viral Zoonotic Disease: Three Years After and Counting
Recent Patents on Anti-Infective Drug Discovery Depression Discovery in Covid-19 Communities Using Deep Learning
Recent Patents on Engineering Novel Anti-Prostate Cancer Curcumin Analogues That Enhance Androgen Receptor Degradation Activity
Anti-Cancer Agents in Medicinal Chemistry Caenorhabditis elegans Databases
Current Genomics Fumagillin and Structurally Related Molecules as Source of New Drugs
Mini-Reviews in Organic Chemistry The Main Receptors Involved in the COVID-19: A Systematic Review and Meta-Analysis
Current Medicinal Chemistry Biological Activities and In Silico Physico-Chemical Properties of 1,2,3- Triazoles Derived from Natural Bioactive Alcohols
Anti-Infective Agents Computational Sampling and Simulation Based Assessment of Novel <i>Mycobacterium tuberculosis</i> Glutamine Synthetase Inhibitors: Study Involving Structure Based Drug Design and Free Energy Perturbation
Current Topics in Medicinal Chemistry How Does the Covıd-19 Pandemıc Affect the Target 90-90-90?
Current HIV Research Tuberculosis, an Old Disease Lacking New Therapeutic Drugs
Current Drug Therapy Vitamin C: Basic Metabolism and Its Function as an Index of Oxidative Stress
Current Medicinal Chemistry A Review of the Rational and Current Evidence on Colchicine for COVID-19
Current Pharmaceutical Design 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 Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse
Mini-Reviews in Medicinal Chemistry Combination of Phytochemicals as Adjuvants for Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery Mechanochemical Synthesis and Reactivity of 1,2,3-Triazole Carbohydrate Derivatives as Glycogen Phosphorylase Inhibitors
Current Organic Synthesis