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Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies
4-Chloro-3-nitrophenylthioureas 1–30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2–64 μg/mL). Among them derivatives with electron-donating alkyl...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222614/ https://www.ncbi.nlm.nih.gov/pubmed/30248936 http://dx.doi.org/10.3390/molecules23102428 |
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author | Bielenica, Anna Sanna, Giuseppina Madeddu, Silvia Giliberti, Gabriele Stefańska, Joanna Kozioł, Anna E. Savchenko, Oleksandra Strzyga-Łach, Paulina Chrzanowska, Alicja Kubiak-Tomaszewska, Grażyna Struga, Marta |
author_facet | Bielenica, Anna Sanna, Giuseppina Madeddu, Silvia Giliberti, Gabriele Stefańska, Joanna Kozioł, Anna E. Savchenko, Oleksandra Strzyga-Łach, Paulina Chrzanowska, Alicja Kubiak-Tomaszewska, Grażyna Struga, Marta |
author_sort | Bielenica, Anna |
collection | PubMed |
description | 4-Chloro-3-nitrophenylthioureas 1–30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2–64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1–6 and 8–19 were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC(50) ≤ 10 μM). The influence of derivatives 11, 13 and 25 on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed. |
format | Online Article Text |
id | pubmed-6222614 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62226142018-11-13 Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies Bielenica, Anna Sanna, Giuseppina Madeddu, Silvia Giliberti, Gabriele Stefańska, Joanna Kozioł, Anna E. Savchenko, Oleksandra Strzyga-Łach, Paulina Chrzanowska, Alicja Kubiak-Tomaszewska, Grażyna Struga, Marta Molecules Article 4-Chloro-3-nitrophenylthioureas 1–30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2–64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1–6 and 8–19 were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC(50) ≤ 10 μM). The influence of derivatives 11, 13 and 25 on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed. MDPI 2018-09-21 /pmc/articles/PMC6222614/ /pubmed/30248936 http://dx.doi.org/10.3390/molecules23102428 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Bielenica, Anna Sanna, Giuseppina Madeddu, Silvia Giliberti, Gabriele Stefańska, Joanna Kozioł, Anna E. Savchenko, Oleksandra Strzyga-Łach, Paulina Chrzanowska, Alicja Kubiak-Tomaszewska, Grażyna Struga, Marta Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title | Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title_full | Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title_fullStr | Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title_full_unstemmed | Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title_short | Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies |
title_sort | disubstituted 4-chloro-3-nitrophenylthiourea derivatives: antimicrobial and cytotoxic studies |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222614/ https://www.ncbi.nlm.nih.gov/pubmed/30248936 http://dx.doi.org/10.3390/molecules23102428 |
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