Synthesis of 1H-1,2,3-Triazole Linked β-Lactam—Isatin Bi-Functional Hybrids and Preliminary Analysis of in vitro Activity Against the Protozoal Parasite Trichomonas vaginalis.

Abstract Twenty-two different triazoles were prepared to examine the anti- Trichomonas vaginalis structure–activity relationships (SAR) within the β-lactam–isatin–triazole conjugate family. The compounds were synthesized by copper-catalyzed ‘click chemistry.’ In vitro activity against T. vaginalis was determined at 10 and 100 μM for each compound, with eighteen of the synthesized hybrids showing 100% growth inhibition at 100 μM. The compound 5i , with no cytotoxicity on cultured CHO-K1 cells, is considered a good compound for further analysis.