2. Academic Validation
  3. Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety

Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety

  • Eur J Med Chem. 2015 Aug 28:101:111-25. doi: 10.1016/j.ejmech.2015.06.027.
Anna Bielenica 1,  Joanna Stefańska 2,  Karolina Stępień 2,  Agnieszka Napiórkowska 3,  Ewa Augustynowicz-Kopeć 3,  Giuseppina Sanna 4,  Silvia Madeddu 4,  Stefano Boi 4,  Gabriele Giliberti 4,  Małgorzata Wrzosek 5,  Marta Struga 5
Affiliations

Affiliations

  • 1 Chair and Department of Biochemistry, Medical University, 02-097 Warszawa, Poland. Electronic address: abielenica@wum.edu.pl.
  • 2 Department of Pharmaceutical Microbiology, Medical University, 02-007 Warszawa, Poland.
  • 3 Department of Microbiology, National Tuberculosis and Lung Diseases Research Institute, 01-138 Warszawa, Poland.
  • 4 Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy.
  • 5 Department of Pharmacogenomics, Faculty of Pharmacy, Medical University, 02-097 Warszawa, Poland.
PMID: 26119992 DOI: 10.1016/j.ejmech.2015.06.027
Abstract

A total of 31 of thiourea derivatives was prepared reacting 3-(trifluoromethyl)aniline and commercial aliphatic and aromatic isothiocyanates. The yields varied from 35% to 82%. All compounds were evaluated in vitro for antimicrobial activity. Derivatives 3, 5, 6, 9, 15, 24 and 27 showed the highest inhibition against Gram-positive cocci (standard and hospital strains). The observed MIC values were in the range of 0.25-16 μg/ml. Inhibitory activity of thioureas 5 and 15 against Topoisomerase IV isolated from Staphylococcus aureus was studied. Products 5 and 15 effectively inhibited the formation of biofilms of methicillin-resistant and standard strains of Staphylococcus epidermidis. Moreover, all obtained thioureas were evaluated for cytotoxicity and Antiviral activity against a large panel of DNA and RNA viruses. Compounds 5, 6, 8-12, 15 resulted cytotoxic against MT-4 cells (CC50 ≤ 10 μM).

Keywords

3-(Trifluoromethyl)aniline; Antimicrobial activity; Biofilm; Cytotoxicity; Thiourea derivatives.

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