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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
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.
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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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