European Journal of Medicinal Chemistry 2015-08-28

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

Anna Bielenica, Joanna Stefańska, Karolina Stępień, Agnieszka Napiórkowska, Ewa Augustynowicz-Kopeć, Giuseppina Sanna, Silvia Madeddu, Stefano Boi, Gabriele Giliberti, Małgorzata Wrzosek, Marta Struga

Index: Eur. J. Med. Chem. 101 , 111-25, (2015)

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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). Copyright © 2015 Elsevier Masson SAS. All rights reserved.