A convenient and efficient synthesis of new triazole β-lactam conjugates using click chemistry is described. β-lactam 15 and 16 were prepared using cycloaddition strategy and propargylated at N-1 to afford compounds 17 and 18. Cu-catalyzed click reaction of these β-lactams 17 and 18 with different aryl azides provided 1,2,3-triazole conjugates 6 and 7, respectively. The products were fully characterized spectroscopically and tested against Gram-(+) and Gram-(-) bacteria. Compound 7a and 7c were found to be most active.
Pharmaceutical chemistry /Microbiology /Triazole /Beta-lactam /Conjugates / Antibacterial assay
Heliyon. 2020 Jun 27;6(6):e04241.doi: 10.1016/j.heliyon.2020.e04241. eCollection 2020 Jun.