ArticleNature2016
A platform for the discovery of new macrolide antibiotics.
Article in Nature, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 132 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.
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Who cites it
132 citing papers in PubMed, 348 citations in OpenAlex.
- Structure-based design and synthesis of group A streptogramins that bind to the nascent peptide exit tunnel of the ribosome.European journal of medicinal chemistry · 2026Article
- Modular Assembly of Macrocyclic Sulfonamides via Consecutive Cascade Ring Expansion Reactions.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Natural Product-Derived Ianthelliformisamines Inhibit Protein Translation and Block Bacterial Flagellum Assembly.ACS chemical biology · 2026Article
- A novel tulathromycin oil suspension injection: preparation, characterization, and pharmacokinetics in goats.BMC veterinary research · 2026Article
- Site-Divergent Oxidations within Venerable Macrolide Antibiotic Scaffolds Unveil Compounds with Broad Spectrum and Anti-MRSA Activities.ACS central science · 2026Article
- PTGS2 as a potential target for apigenin to promote spinal cord injury repair.Journal of bioenergetics and biomembranes · 2026Article
- Evolution of a Strategy for the Unified Synthesis of Enteropeptin Sactipeptides.The Journal of organic chemistry · 2026Article
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- Anti-infective macrozones: design, biological evaluation and structure-activity relationships.ADMET & DMPK · 2026Article
- Hybrid Antibiotics Targeting the Bacterial Ribosome.ACS central science · 2025Article
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- Engineering the Specificity of Acetyl-CoA Synthetase for Diverse Acyl-CoA Thioester Generation.ACS chemical biology · 2025Article
- Directed Evolution of a Macrolide-Sensing Transcription Factor Biosensor for the Detection of Macrolactone Aglycones via "Effector Walking" and Efflux Pump Deletion.Biochemistry · 2025Article
- Creation of a macrolide antibiotic against non-tuberculousScience advances · 2025Article
- Fast Esterification Method Mediated by Coupling Reagent NDTP.ACS omega · 2025Article
- Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research.Angewandte Chemie (International ed. in English) · 2025Review
- Stereoselective Synthesis of Benzoylated Gulmirecin A and Disciformycin B.Organic letters · 2025Article
- Directed Evolution of a Modular Polyketide Synthase Thioesterase for Generation of a Hybrid Macrocyclic Ring System.ACS catalysis · 2025Article
- Refactoring the pikromycin synthase for the modular biosynthesis of macrolide antibiotics in E. coli.Research square · 2025Article
- Antimicrobial peptides: natural templates for next-generation therapeutics against antimicrobial resistance.Frontiers in cellular and infection microbiology · 2025Review
72 more citing papers are in PubMed but not listed here.
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Authors and funding
16 authors at 1 institution in 1 country.
Funding
Abstract
The chemical modification of structurally complex fermentation products, a process known as semisynthesis, has been an important tool in the discovery and manufacture of antibiotics for the treatment of various infectious diseases. However, many of the therapeutics obtained in this way are no longer effective, because bacterial resistance to these compounds has developed. Here we present a practical, fully synthetic route to macrolide antibiotics by the convergent assembly of simple chemical building blocks, enabling the synthesis of diverse structures not accessible by traditional semisynthetic approaches. More than 300 new macrolide antibiotic candidates, as well as the clinical candidate solithromycin, have been synthesized using our convergent approach. Evaluation of these compounds against a panel of pathogenic bacteria revealed that the majority of these structures had antibiotic activity, some efficacious against strains resistant to macrolides in current use. The chemistry we describe here provides a platform for the discovery of new macrolide antibiotics and may also serve as the basis for their manufacture.
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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.