ArticleJournal of medicinal chemistry2015
Synthesis and evaluation of 1,2,4-triazolo[1,5-a]pyrimidines as antibacterial agents against Enterococcus faecium.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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
20 citing papers in PubMed, 108 citations in OpenAlex.
- Antidiabetic Evaluation of New Pyrimidine-Thiazoline Hybrids Endorsed With Enzyme Kinetic Studies and Computational Analysis.Chemical biology & drug design · 2025Article
- An Engineered Nisin Analogue with a Hydrophobic Moiety Attached at Position 17 Selectively InhibitsACS chemical biology · 2024Article
- The preparation of [1,2,4]triazolo[1,5-RSC advances · 2024Article
- First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Design, Synthesis and Biological Evaluation of [1,2,4]Triazolo[1,5-Molecules (Basel, Switzerland) · 2022Article
- Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids.ACS medicinal chemistry letters · 2022Article
- Oxidative Aromatization of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines: Synthetic Possibilities and Limitations, Mechanism of Destruction, and the Theoretical and Experimental Substantiation.Molecules (Basel, Switzerland) · 2021Article
- Design, synthesis, crystal structure and in vitro antimicrobial activity of novel 1,2,4-triazolo[1,5-a]pyrimidine-containing quinazolinone derivatives.Molecular diversity · 2021Article
- Unconventional Antibacterials and Adjuvants.Accounts of chemical research · 2021Article
- Interplay between ESKAPE Pathogens and Immunity in Skin Infections: An Overview of the Major Determinants of Virulence and Antibiotic Resistance.Pathogens (Basel, Switzerland) · 2021Review
- Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-RSC advances · 2021Article
- A novel protocol for catalyst-free synthesis of fused six-member rings to triazole and pyrazole.Molecular diversity · 2020Article
- 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.European journal of medicinal chemistry · 2019Review
- Triazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors.Bioorganic & medicinal chemistry letters · 2019Article
- 3-Dialkylamino-1,2,4-triazoles via ZnACS omega · 2018Article
- A Greener and Efficient Method for Nucleophilic Aromatic Substitution of Nitrogen-Containing Fused Heterocycles.Molecules (Basel, Switzerland) · 2018Article
- Aminoazole-Based Diversity-Oriented Synthesis of Heterocycles.Frontiers in chemistry · 2018Review
- Narrow-Spectrum Antibacterial Agents.MedChemComm · 2018Article
- The Natural Product Essramycin and Three of Its Isomers Are Devoid of Antibacterial Activity.Journal of natural products · 2016Article
- Exploration of the structure-activity relationship of 1,2,4-oxadiazole antibiotics.Bioorganic & medicinal chemistry letters · 2015Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Rapid emergence of antibiotic resistance is one of the most challenging global public health concerns. In particular, vancomycin-resistant Enterococcus faecium infections have been increasing in frequency, representing 25% of enterococci infections in intensive care units. A novel class of 1,2,4-triazolo[1,5-a]pyrimidines active against E. faecium is reported herein. We used a three-component Biginelli-like heterocyclization reaction for the synthesis of a series of these derivatives based on reactions of aldehydes, β-dicarbonyl compounds, and 3-alkylthio-5-amino-1,2,4-triazoles. The resulting compounds were assayed for antimicrobial activity against the ESKAPE panel of bacteria, followed by investigation of their in vitro activities. These analyses identified a subset of 1,2,4-triazolo[1,5-a]pyrimidines that had good narrow-spectrum antibacterial activity against E. faecium and exhibited metabolic stability with low intrinsic clearance. Macromolecular synthesis assays revealed cell-wall biosynthesis as the target of these antibiotics.
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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.