ArticleTetrahedron letters2018
Amidation Strategy for Final-Step α-Hydroxytropolone Diversification.
Article in Tetrahedron letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Liquid-Phase Peptide Synthesis of Tropolone-Peptide Hybrid Antimalarials.Organic letters · 2026Article
- Targeting Metalloenzymes: The "Achilles' Heel" of Viruses and Parasites.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Antiviral activity of amide-appended α-hydroxytropolones against herpes simplex virus-1 and -2.RSC advances · 2023Article
- Carbocycloaddition Strategies for Troponoid Synthesis.Tetrahedron · 2023Article
- Synthesis of α-Tropolones through Autoxidation of Dioxole-Fused Cycloheptatrienes.The Journal of organic chemistry · 2022Article
- Synthesis of Polyoxygenated Tropolones and their Antiviral Activity against Hepatitis B Virus and Herpes Simplex Virus-1.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Article
- Recent Advances in Hepatitis B Treatment.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Investigations into a Stoichiometrically Equivalent Intermolecular Oxidopyrylium [5 + 2] Cycloaddition Reaction Leveraging 3-Hydroxy-4-pyrone-Based Oxidopyrylium Dimers.The Journal of organic chemistry · 2021Article
- Amide-containing α-hydroxytropolones as inhibitors of hepatitis B virus replication.Antiviral research · 2020Article
- Synthesis of aryl-substituted 2-methoxyphenol derivatives from maltol-derived oxidopyrylium cycloadducts through an acid-mediated ring contraction cascade.Chemical communications (Cambridge, England) · 2020Article
- Spectrophotometric determination of α-hydroxytropolone pTetrahedron letters · 2019Article
- Troponoid Atropisomerism: Studies on the Configurational Stability of Tropone-Amide Chiral Axes.Organic letters · 2019Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
α-Hydroxytropolones (αHTs) are excellent metalloenzyme-inhibiting fragments that have been the basis for the development of potent inhibitors of various therapeutically important enzymes. The following manuscript describes a final-step amidation approach for αHT diversification. The method takes advantage of a scalable, chromatography-free synthesis of a carboxylic acid-appended αHT, and in the present manuscript we describe the synthesis of eight amide-containing αHTs, three of which we envision using as chemical probes. We expect that the general strategy will find widespread usage in both chemical biology and medicinal chemistry studies on αHTs.
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