13628-29-0Relevant academic research and scientific papers
5-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives
Bielenica, Anna,K?dzierska, Ewa,Koliński, Micha?,Kmiecik, Sebastian,Koliński, Andrzej,Fiorino, Ferdinando,Severino, Beatrice,Magli, Elisa,Corvino, Angela,Rossi, Ilaria,Massarelli, Paola,Kozio?, Anna E.,Sawczenko, Aleksandra,Struga, Marta
, p. 173 - 186 (2016)
A series of 10 thiourea derivatives have been synthesized by the reaction of aromatic amine with a substituted aryl (compounds 1-3, 6-8) and alkylphenyl (4, 5, 9, 10) isothiocyanates. Their in vitro and in vivo pharmacological properties were studied. Amo
1H-Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies
Bielenica, Anna,Szulczyk, Daniel,Olejarz, Wioletta,Madeddu, Silvia,Giliberti, Gabriele,Materek, Ilona B.,Koziol, Anna E.,Struga, Marta
, p. 804 - 812 (2017)
On the basis of recently reported biologically active 3-(trifluoromethyl)phenylthioureas, a series of diaryl derivatives incorporating 1H-tetrazol-5-yl (1a–11a, 1a’–11a’) and 1,3-thiazolidin-4-one (1b–11b) scaffolds were synthesized. The synthesis pathway
Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety
Bielenica, Anna,Stefanska, Joanna,Stepien, Karolina,Napiorkowska, Agnieszka,Augustynowicz-Kopec, Ewa,Sanna, Giuseppina,Madeddu, Silvia,Boi, Stefano,Giliberti, Gabriele,Wrzosek, Malgorzata,Struga, Marta
, p. 111 - 125 (2015/06/30)
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 0.25e16 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, 8e12, 15 resulted cytotoxic against MT-4 cells (CC50≤ 10μM).
