|SINGH, AMANDEEP - Guru Nanak Dev University|
|ZHANG, DAVID - University Of The Pacific|
|Cheng, Luisa Wai Wai|
|LAND, KIRKWOOD - University Of The Pacific|
|KUMAR, VIPAN - Guru Nanak Dev University|
Submitted to: Bioorganic and Medicinal Chemistry Letters
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 5/25/2019
Publication Date: 5/30/2019
Citation: Singh, A., Zhang, D., Tam, C.C., Cheng, L.W., Land, K.M., Kumar, V. 2019. Synthesis and antiprotozoal activity of functionalized 1H-1,2,3-triazole-tethered isatin-ferrocene conjugates. Bioorganic and Medicinal Chemistry Letters. 896:1-4. https://doi.org/10.1016/j.jorganchem.2019.05.025.
Interpretive Summary: Identifying potential new therapies against infectious diseases is critical to human and animal health. In this study, copper-promoted isatin-conjugates compounds were synthesized and tested them against the human pathogen Trichomonas vaginalis. Our results identified several lead compounds against this eukaryotic pathogen. Since antibiotics often negatively impact the normal flora of a patient, we also screened the chemical library on several known normal flora bacteria and observed no effect on their growth at the highest concentration used in this study. Taken together, this study has identified several possible new leads for drug discovery against Trichomonas vaginalis.
Technical Abstract: Copper-promoted azide-alkyne cycloadditions were attempted to synthesize a series of variedly functionalized 1H-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 are specific against trichomonad protozoa.