Synthesis and biological evaluation of some new β-lactam-triazole hybrids

Synthesis and biological evaluation of some new β-lactam-triazole hybrids

A series of novel β-lactams was synthesized from different imines and a special ketene derived from N -endo-5-norbornene-2,3-dicarboxyloylglycine 1 via the [2 + 2] ketene imine cycloaddition. Then, β-lactams 3a – h were treated with 1-azido-4-nitrobenzene 4 to afford β-lactam-triazole hybrids 5a – h...

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Veröffentlicht in:Medicinal chemistry research 2016, Vol.25 (1), p.149-162
Hauptverfasser: Jarrahpour, Aliasghar, Shirvani, Pouria, Sinou, Véronique, Latour, Christine, Brunel, Jean M.
Format: Artikel
Sprache:eng
Schlagworte:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
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Zusammenfassung:A series of novel β-lactams was synthesized from different imines and a special ketene derived from N -endo-5-norbornene-2,3-dicarboxyloylglycine 1 via the [2 + 2] ketene imine cycloaddition. Then, β-lactams 3a – h were treated with 1-azido-4-nitrobenzene 4 to afford β-lactam-triazole hybrids 5a – h . Of the twenty-three β-lactams tested against chloroquine-resistant P. falciparum K14 strain, 3a and 3d showed IC 50  
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-015-1474-x