ArticleThe Journal of antibiotics2018
Discovery of hybrids of indolin-2-one and nitroimidazole as potent inhibitors against drug-resistant bacteria.
Article in The Journal of antibiotics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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Who cites it
8 citing papers in PubMed, 18 citations in OpenAlex.
- Prominent mediatory role of gut microbiome in the effect of lifestyle on host metabolic phenotypes.Gut microbes · 2025Article
- Synthesis and Antimicrobial Activity of 3-Alkylidene-2-Indolone Derivatives.Molecules (Basel, Switzerland) · 2024Article
- Article
- Indolin-2-one Nitroimidazole Antibiotics Exhibit an Unexpected Dual Mode of Action.ACS chemical biology · 2022Article
- An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety.Molecules (Basel, Switzerland) · 2020Review
- Design and synthesis of novel spirooxindole-indenoquinoxaline derivatives as novel tryptophanyl-tRNA synthetase inhibitors.Molecular diversity · 2020Article
- A Novel Small Molecule, ZY354, Inhibits Dental Caries-Associated Oral Biofilms.Antimicrobial agents and chemotherapy · 2019Article
- Multicomponent reactions (MCRs): a useful access to the synthesis of benzo-fused γ-lactams.Beilstein journal of organic chemistry · 2019Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
With antibiotics resistance developing rapidly, new antibacterial agents are needed to be discovered. We readily synthesized 11 indolin-2-one compounds and found a hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)indolin-2-one to be effective on Staphylococcus aureus strains. Six derivatives of this compound were further designed and synthesized in order to enhance its efficacy. After a second turn of structural refinement, a novel hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)-5-nitroindolin-2-one with a nitro group on C-5 position of indolin-2-one was shown to exhibit remarkable antibacterial activities with a low MIC value against MRSA ATCC 33591. Besides, this molecule demonstrated its potency on Gram-negative bacteria and VRE strain. The time-killing curve experiment showed its good bactericidal activity. Low hemolytic rate suggested its promising safety profile.
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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.