Click-chemistry approach to synthesis of functionalized isatin-ferrocenes and their biological evaluation against the human pathogen Trichomonas vaginalis.

Copper-promoted azide-alkyne cycloadditions were attempted to synthesize a series of variedly functionalized 1 H -1,2,3-triazole-linked isatin-ferrocene, ferrocenylmethoxy-isatin and isatin-ferrocenyl-chalcone conjugates. The synthesized scaffolds were assayed for their inhibitory activity against T. vaginalis as well as several common normal human flora bacteria. The observed inhibitory activities against T. vaginalis and undetectable inhibition of microflora bacteria suggest that these compounds may be specific against trichomonad protozoa and could serve as a new scaffold for synthesis of novel compounds against this important human pathogen. Image 1 • Synthesis and anti trichomonad evaluation of isatin-ferrocene conjugates. • The presence of halogen at C-5 position proved to be essential for good activities. • The conjugate 11f displayed an IC 50 value of 27 μM and was non-cytotoxic. [ABSTRACT FROM AUTHOR]