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• W2080383657 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." @default.
• W2080383657 created "2016-06-24" @default.
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• W2080383657 date "2015-05-12" @default.
• W2080383657 modified "2023-10-11" @default.
• W2080383657 title "Synthesis and Evaluation of 1,2,4-Triazolo[1,5-<i>a</i>]pyrimidines as Antibacterial Agents Against <i>Enterococcus faecium</i>" @default.
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• W2080383657 doi "https://doi.org/10.1021/jm501831g" @default.
• W2080383657 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4633020" @default.
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