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

[Image: see text] 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 synthes...

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Autores principales: Singh, Amandeep, Fong, Grant, Liu, Jenny, Wu, Yun-Hsuan, Chang, Kevin, Park, William, Kim, Jihwan, Tam, Christina, Cheng, Luisa W., Land, Kirkwood M., Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6045481/
https://www.ncbi.nlm.nih.gov/pubmed/30023926
http://dx.doi.org/10.1021/acsomega.8b00553
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author Singh, Amandeep
Fong, Grant
Liu, Jenny
Wu, Yun-Hsuan
Chang, Kevin
Park, William
Kim, Jihwan
Tam, Christina
Cheng, Luisa W.
Land, Kirkwood M.
Kumar, Vipan
author_facet Singh, Amandeep
Fong, Grant
Liu, Jenny
Wu, Yun-Hsuan
Chang, Kevin
Park, William
Kim, Jihwan
Tam, Christina
Cheng, Luisa W.
Land, Kirkwood M.
Kumar, Vipan
author_sort Singh, Amandeep
collection PubMed
description [Image: see text] 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. IC(50) 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.
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spelling pubmed-60454812018-07-16 Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates Singh, Amandeep Fong, Grant Liu, Jenny Wu, Yun-Hsuan Chang, Kevin Park, William Kim, Jihwan Tam, Christina Cheng, Luisa W. Land, Kirkwood M. Kumar, Vipan ACS Omega [Image: see text] 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. IC(50) 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. American Chemical Society 2018-05-30 /pmc/articles/PMC6045481/ /pubmed/30023926 http://dx.doi.org/10.1021/acsomega.8b00553 Text en Copyright © 2018 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Singh, Amandeep
Fong, Grant
Liu, Jenny
Wu, Yun-Hsuan
Chang, Kevin
Park, William
Kim, Jihwan
Tam, Christina
Cheng, Luisa W.
Land, Kirkwood M.
Kumar, Vipan
Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title_full Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title_fullStr Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title_full_unstemmed Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title_short Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
title_sort synthesis and preliminary antimicrobial analysis of isatin–ferrocene and isatin–ferrocenyl chalcone conjugates
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6045481/
https://www.ncbi.nlm.nih.gov/pubmed/30023926
http://dx.doi.org/10.1021/acsomega.8b00553
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