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New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications

Department of Pharmaceutical Chemistry, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Department of Microbiology, Faculty of Biology & Research Institute of the University of Bucharest (ICUB), University of Bucharest, 060101 Bucharest, Romania
The Organic Chemistry Center of Romanian Academy “C. D. Neniţescu”, 060023 Bucharest, Romania
Inorganic Chemistry Department, Faculty of Chemistry, University of Bucharest, 020462 Bucharest, Romania
National Institute of Chemical-Pharmaceutical Research & Development, 031299 Bucharest, Romania
Stefan S. Nicolau Institute of Virology, Mihai Bravu 285, Bucharest, 030304, Romania
Author to whom correspondence should be addressed.
Molecules 2020, 25(7), 1478;
Received: 21 February 2020 / Revised: 18 March 2020 / Accepted: 20 March 2020 / Published: 25 March 2020
(This article belongs to the Special Issue Organofluorine Chemistry)
The increasing threat of antimicrobial resistance to all currently available therapeutic agents has urged the development of novel antimicrobials. In this context, a series of new benzoylthiourea derivatives substituted with one or more fluorine atoms and with the trifluoromethyl group have been tested, synthesized, and characterized by IR, NMR, CHNS and crystal X-ray diffraction. The molecular docking has provided information regarding the binding affinity and the orientation of the new compounds to Escherichia coli DNA gyrase B. The docking score predicted the antimicrobial activity of the studied compounds, especially against E. coli, which was further demonstrated experimentally against planktonic and biofilm embedded bacterial and fungal cells. The compounds bearing one fluorine atom on the phenyl ring have shown the best antibacterial effect, while those with three fluorine atoms exhibited the most intensive antifungal activity. All tested compounds exhibited antibiofilm activity, correlated with the trifluoromethyl substituent, most favorable in para position. View Full-Text
Keywords: benzoylthiourea derivatives; antimicrobial; antibiofilm; X-ray; in silico benzoylthiourea derivatives; antimicrobial; antibiofilm; X-ray; in silico
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Limban, C.; Chifiriuc, M.C.; Caproiu, M.T.; Dumitrascu, F.; Ferbinteanu, M.; Pintilie, L.; Stefaniu, A.; Vlad, I.M.; Bleotu, C.; Marutescu, L.G.; Nuta, D.C. New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications. Molecules 2020, 25, 1478.

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