ArticleJournal of medicinal chemistry2016
1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists.
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
What it found
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The trial behind it
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Who cites it
36 citing papers in PubMed.
- Click Chemistry Approach to Derivatisation of Fluconazole.Molecules (Basel, Switzerland) · 2026Article
- Pharmacology of estrogen-related receptors (ERRs) agonists.RSC chemical biology · 2026Review
- 4-Sulfanyl-1,2,3-triazole as a Powerful Ligand in CuAAC to Synthesize 1,4-Substituted 1,2,3-Triazoles Under Solvent-Free and Low Catalyst Loading.Molecules (Basel, Switzerland) · 2026Article
- Density Function Theory Study on the Energy and Circular Dichroism Spectrum for Methylene-Linked Triazole Diads Depending on the Substitution Position and Conformation.Molecules (Basel, Switzerland) · 2024Article
- Article
- Average Electron Density: A Quantitative Tool for Evaluating Non-Classical Bioisosteres of Amides.ACS omega · 2024Article
- Novel Bis-1,2,3-triazole-thiazolidinone hybrid as anticancer agents that induce apoptosis and molecular modeling study.Future medicinal chemistry · 2024Article
- Article
- Red light-emitting short Mango-based system enables tracking a mycobacterial small noncoding RNA in infected macrophages.Nucleic acids research · 2023Article
- Advances in the Synthesis of Fused 1,2,3-Triazoles via a MCR-Intramolecular Azide-Alkyne Cycloaddition Approach.Molecules (Basel, Switzerland) · 2022Review
- Design, Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2022Article
- Selective Synthesis of AzoloylACS omega · 2022Article
- Chiral Cyclic Aliphatic Linkers as Building Blocks for Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Evaluation of Amide Bioisosteres Leading to 1,2,3-Triazole Containing Compounds as GPR88 Agonists: Design, Synthesis, and Structure-Activity Relationship Studies.Journal of medicinal chemistry · 2021Article
- In vitro anti-Toxoplasma gondii efficacy of synthesised benzyltriazole derivatives.The Onderstepoort journal of veterinary research · 2021Article
- Structure property relationships of N-acylsulfonamides and related bioisosteres.European journal of medicinal chemistry · 2021Article
- Multifaceted HIV-1 Vif interactions with human E3 ubiquitin ligase and APOBEC3s.The FEBS journal · 2021Article
- Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.Journal of medicinal chemistry · 2021Article
- Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.ACS medicinal chemistry letters · 2021Article
- Potential Utilization of APOBEC3-Mediated Mutagenesis for an HIV-1 Functional Cure.Frontiers in microbiology · 2021Review
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
RN-18 based viral infectivity factor (Vif), Vif antagonists reduce viral infectivity by rescuing APOBEC3G (A3G) expression and enhancing A3G-dependent Vif degradation. Replacement of amide functionality in RN-18 (IC50 = 6 μM) by isosteric heterocycles resulted in the discovery of a 1,2,3-trizole, 1d (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a 1d based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μM).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.