ArticleAngewandte Chemie (International ed. in English)2023
High-Throughput Diversification of Complex Bioactive Molecules by Accelerated Synthesis in Microdroplets.
Article in Angewandte Chemie (International ed. in English), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed.
- Accelerated Chemistry in Microdroplets.Accounts of chemical research · 2026Article
- Early-stage drug discovery in a new-generation ultrahigh-throughput mass spectrometry platform.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Characterization of blood serum and cell lines by an automated high-throughput well plate sampling system using laser ablation-rapid evaporative ionization mass spectrometry.Analytical and bioanalytical chemistry · 2026Article
- Advances in natural product discovery: strategies, technologies, and insights.Natural products and bioprospecting · 2026Review
- Recent Advances in Reactive Microdroplets for Clean Water and Energy.Advanced materials (Deerfield Beach, Fla.) · 2025Review
- Ambient ionization mass spectrometry in brain cancer diagnosis.Journal of mass spectrometry and advances in the clinical lab · 2025Review
- High-Throughput Small-Scale Platform for Synthesis, Characterization, and Modeling of Per- and Polyfluoroalkyl Substances Analogs.Environmental science & technology letters · 2025Article
- Mechanisms of ionization and of chemical reactions in charged microdroplets.Chemical science · 2025Review
- Accelerating countermeasure candidate discovery for A-series chemical warfare agent exposure.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- High-Throughput Drug Derivatization and Bioassay by Desorption Electrospray Ionization Mass Spectrometry.ChemPlusChem · 2025Article
- Why do some metal ions spontaneously form nanoparticles in water microdroplets? Disentangling the contributions of the air-water interface and bulk redox chemistry.Chemical science · 2025Article
- Diversity Oriented Clicking for Modular Synthesis.Nature reviews. Methods primers · 2025Article
- The gas|liquid interface eclipses the liquid|liquid interface for glucose oxidase rate acceleration in microdroplets.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Rapid Exploration of Chemical Space by High-Throughput Desorption Electrospray Ionization Mass Spectrometry.Journal of the American Chemical Society · 2024Article
- High-Throughput Assessment of Bile Salt Export Pump Inhibition Using RapidFire-MS and DESI-MS.ACS medicinal chemistry letters · 2024Article
- Reaction acceleration at the surface of a levitated droplet by vapor dosing from a partner droplet.Chemical science · 2024Article
- High-throughput label-free opioid receptor binding assays using an automated desorption electrospray ionization mass spectrometry platform.Chemical communications (Cambridge, England) · 2024Article
- Desorption Electrospray Ionization Mass Spectrometry: 20 Years.Accounts of chemical research · 2023Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
Late-stage diversification of drug molecules is an important strategy in drug discovery that can be facilitated by reaction screening using high-throughput experimentation. Here we present a rapid method for functionalizing bioactive molecules based on accelerated reactions in microdroplets. Reaction mixtures are nebulized at throughputs better than 1 reaction/second and the accelerated reactions occurring in the microdroplets are followed by desorption electrospray ionization mass spectrometry (DESI-MS). Because the accelerated reactions occur on the millisecond timescale, they allow an overall screening throughput of 1 Hz working at the low nanogram scale. Using this approach, an opioid agonist (PZM21) and an antagonist (naloxone) were diversified using three reactions important in medicinal chemistry: sulfur fluoride exchange (SuFEx) click reactions, imine formation reactions, and ene-type click reactions. Some 269 functionalized analogs of naloxone and PZM21 were generated and characterized by tandem mass spectrometry (MS/MS) after screening over 500 reactions.
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What Socratic holds
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 Socratic graph.