ArticleProceedings of the National Academy of Sciences of the United States of America2013
Bio-inspired synthesis yields a tricyclic indoline that selectively resensitizes methicillin-resistant Staphylococcus aureus (MRSA) to β-lactam antibiotics.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 120 citations in OpenAlex.
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- A small-molecule membrane fluidizer re-sensitizes methicillin-resistantAntimicrobial agents and chemotherapy · 2023Article
- Dearomative (3+2) Cycloadditions between Indoles and Vinyldiazo Species Enabled by a Red-Shifted Chromium Photocatalyst.Angewandte Chemie (International ed. in English) · 2022Article
- Entropy-Induced Selectivity Switch in Gold Catalysis: Fast Access to Indolo[1,2-a]quinolines.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Structure-activity relationship studies of [1,2,5]oxadiazolo[3,4-b]pyrazine-containing polymyxin-selective resistance-modifying agents.Bioorganic & medicinal chemistry letters · 2022Article
- Serendipitous Discovery of a Highly Active and Selective Resistance-Modifying Agent for Colistin-Resistant Gram-Negative Bacteria.ACS omega · 2022Article
- Synergistic action of substituted indole derivatives and clinically used antibiotics against drug-resistant bacteria.Future microbiology · 2020Article
- Modular Synthesis of Polycyclic Alkaloid Scaffolds via an Enantioselective Dearomative Cascade.Organic letters · 2020Article
- Recent Advances in Construction of Polycyclic Natural Product Scaffolds via One-Pot Reactions Involving Alkyne Annulation.Frontiers in chemistry · 2020Review
- Anthracycline Shunt Metabolites From Philippine Marine Sediment-DerivedFrontiers in microbiology · 2020Article
- Tryptoline-based benzothiazoles re-sensitize MRSA to β-lactam antibiotics.Bioorganic & medicinal chemistry · 2019Article
- Zn(OTf)Chemical science · 2019Article
- Rh(iii)-catalyzed C-7 arylation of indolines with arylsilanesRSC advances · 2019Article
- Photoactivated 2,3-distyrylindoles kill multi-drug resistant bacteria.Bioorganic & medicinal chemistry letters · 2018Article
- Enantioselective Tandem Cyclization of Alkyne-Tethered Indoles Using Cooperative Silver(I)/Chiral Phosphoric Acid Catalysis.Angewandte Chemie (International ed. in English) · 2017Article
- Diastereoselective synthesis and biological evaluation of enantiomerically pure tricyclic indolines.Organic & biomolecular chemistry · 2017Article
- A Tryptoline Ring-Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Tetracyclic indolines as a novel class of β-lactam-selective resistance-modifying agent for MRSA.European journal of medicinal chemistry · 2017Article
- Construction of spirocarbocyclesChemical science · 2016Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The continuous emergence of resistant bacteria has become a major worldwide health threat. The current development of new antibacterials has lagged far behind. To discover reagents to fight against resistant bacteria, we initiated a chemical approach by synthesizing and screening a small molecule library, reminiscent of the polycyclic indole alkaloids. Indole alkaloids are a class of structurally diverse natural products, many of which were isolated from plants that have been used as traditional medicine for millennia. Specifically, we adapted an evolutionarily conserved biosynthetic strategy and developed a concise and unified diversity synthesis pathway. Using this pathway, we synthesized 120 polycyclic indolines that contain 26 distinct skeletons and a wide variety of functional groups. A tricyclic indoline, Of1, was discovered to selectively potentiate the activity of β-lactam antibiotics in multidrug-resistant methicillin-resistant Staphylococcus aureus (MRSA), but not in methicillin-sensitive S. aureus. In addition, we found that Of1 itself does not have antiproliferative activity but can resensitize several MRSA strains to the β-lactam antibiotics that are widely used in the clinic, such as an extended-spectrum β-lactam antibiotic amoxicillin/clavulanic acid and a first-generation cephalosporin cefazolin. These data suggest that Of1 is a unique selective resistance-modifying agent for β-lactam antibiotics, and it may be further developed to fight against resistant bacteria in the clinic.
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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.