Bielenica Anna, Stefańska Joanna, Stępień Karolina, Napiórkowska Agnieszka, Augustynowicz-Kopeć Ewa, Sanna Giuseppina, Madeddu Silvia, Boi Stefano, Giliberti Gabriele, Wrzosek Małgorzata, Struga Marta
Chair and Department of Biochemistry, Medical University, 02-097 Warszawa, Poland.
Department of Pharmaceutical Microbiology, Medical University, 02-007 Warszawa, Poland.
Eur J Med Chem. 2015 Aug 28;101:111-25. doi: 10.1016/j.ejmech.2015.06.027. Epub 2015 Jun 14.
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).
通过使3-(三氟甲基)苯胺与市售脂肪族和芳香族异硫氰酸酯反应，总共制备了31种硫脲衍生物。产率在35%至82%之间。对所有化合物进行了体外抗菌活性评估。衍生物3、5、6、9、15、24和27对革兰氏阳性球菌（标准菌株和医院菌株）表现出最高抑制作用。观察到的最低抑菌浓度值在0.25 - 16μg/ml范围内。研究了硫脲5和15对从金黄色葡萄球菌分离的拓扑异构酶IV的抑制活性。产物5和15有效抑制了耐甲氧西林表皮葡萄球菌和标准菌株生物膜的形成。此外，对所有得到的硫脲针对大量DNA和RNA病毒进行了细胞毒性和抗病毒活性评估。化合物5、6、8 - 12、15对MT - 4细胞具有细胞毒性（半数细胞毒性浓度≤10μM）。
