title: Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety.
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).
authors.affiliation: Chair and Department of Biochemistry, Medical University, 02-097 Warszawa, Poland. Electronic address: abielenica@wum.edu.pl.
authors.forename: Anna
authors.initials: A
authors.lastname: Bielenica
authors.affiliation: Department of Pharmaceutical Microbiology, Medical University, 02-007 Warszawa, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Stefańska
authors.affiliation: Department of Pharmaceutical Microbiology, Medical University, 02-007 Warszawa, Poland.
authors.forename: Karolina
authors.initials: K
authors.lastname: Stępień
authors.affiliation: Department of Microbiology, National Tuberculosis and Lung Diseases Research Institute, 01-138 Warszawa, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiórkowska
authors.affiliation: Department of Microbiology, National Tuberculosis and Lung Diseases Research Institute, 01-138 Warszawa, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopeć
authors.affiliation: Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy.
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.affiliation: Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Madeddu
authors.affiliation: Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Boi
authors.affiliation: Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy.
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.affiliation: Department of Pharmacogenomics, Faculty of Pharmacy, Medical University, 02-097 Warszawa, Poland.
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Wrzosek
authors.affiliation: Department of Pharmacogenomics, Faculty of Pharmacy, Medical University, 02-097 Warszawa, Poland.
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
mesh_terms: D000814:Aniline Compounds / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D059003:Topoisomerase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000814:Aniline Compounds; D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D059003:Topoisomerase Inhibitors; D027101:DNA Topoisomerase IV; D013890:Thiourea
keywords: 3-(Trifluoromethyl)aniline; Antimicrobial activity; Biofilm; Cytotoxicity; Thiourea derivatives