Molecules
Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali, University of Messina, Via S.S. Annunziata, 98168 Messina, Italy.
Published: July 2018
Pyrimidine-1,3-oxazolidin-2-arylimino hybrids have been synthesized as a new class of antibacterial agents. The synthetic approach exploits a Cu(II)-catalyzed intramolecular halkoxyhalogenation of alkynyl ureas, followed by a Suzuki coupling reaction with 2,4-dimethoxypyrimidin-5-boronic acid. Biological screenings revealed that most of the compounds showed moderate to good activity against two Gram-positive (, ) and three Gram-negative (, , ) pathogenic strains. A molecular docking study, performed in the crystal structure of 50S ribosomal unit of indicated that pyrimidine-oxazolidin-2-arylimino hybrids and exhibited a high binding affinity (-9.65 and -10.74 kcal/mol), which was in agreement with their good antibacterial activity. The obtained results suggest that the combination of pyrimidine and oxazolidone moieties can be considered as a valid basis to develop new further modifications towards more efficacious antibacterial compounds.
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Source |
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099984 | PMC |
http://dx.doi.org/10.3390/molecules23071754 | DOI Listing |
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