Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam-isatin conjugates against the human protozoal pathogen Trichomonas vaginalis.

ABSTRACT: In this study, we describe the synthesis of mono- and bis-1H-1,2,3-triazole-tethered β-lactam-isatin conjugates using copper-catalysed azide-alkyne cycloaddition reaction between mono- and di-propargylated azetidin-2-ones and N-alkylazido isatins. The synthesized conjugates were evaluated for their preliminary in vitro analysis against Trichomonas vaginalis at 50 μM. The efficacy of synthesized hybrids was observed to depend on the substituent at N-1 position of β-lactam ring, as well as the presence of single/double 1H-1,2,3-triazole linker. Among the synthesized conjugates, the presence of a p-tolyl substituent at N-1 of β-lactam ring was preferred for good activity profiles while the increase in spacer length did not influence the efficac

SUBMITTER: Raj R 

PROVIDER: S-EPMC7080013 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature