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Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates

Author:
Amandeep Singh, Grant Fong, Jenny Liu, Yun-Hsuan Wu, Kevin Chang, William Park, Jihwan Kim, Christina Tam, Luisa Cheng, Kirkwood Land, Vipan Kumar
Source:
ACS omega 2018 v.3 no.5 pp. 5808-5813
ISSN:
2470-1343
Subject:
Trichomonas vaginalis, antiprotozoal properties, chalcone, ferrocenes, indoles, inhibitory concentration 50, microbiome, synthesis, triazoles, trichomoniasis
Abstract:
In this study, we outline the synthesis of isatin–ferrocenyl chalcone and 1H-1,2,3-triazole-tethered isatin–ferrocene conjugates along with their antimicrobial evaluation against the human mucosal pathogen Trichomonas vaginalis. The introduction of a triazole ring among the synthesized conjugates improved the activity profiles with most of the compounds in the library, exhibiting 100% growth inhibition in a preliminary susceptibility screen at 100 μM. IC50 determination of the most potent compounds in the set revealed an inhibitory range between 2 and 13 μM. Normal flora microbiome are unaffected by these compounds, suggesting that these may be new chemical scaffolds for the discovery of new drugs against trichomonad infections.
Agid:
6473320
Handle:
10113/6473320