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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...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2018
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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. |
format | Online Article Text |
id | pubmed-6045481 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
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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