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Title: | Pentafluorosulfanyl-containing Triclocarban Analogs with Potent Antimicrobial Activity |
Author: | Pujol, Eugènia Blanco-Cabra, Núria Julián, Esther Leiva Martínez, Rosana Torrents Serra, Eduard Vázquez Cruz, Santiago |
Keywords: | Medicaments antibacterians Citotoxicitat per mediació cel·lular Disseny de medicaments Síntesi orgànica Estafilococs Antibacterial agents Cell-mediated cytotoxicity Drug design Organic synthesis Staphylococcus |
Issue Date: | 2-Nov-2018 |
Publisher: | MDPI |
Abstract: | Concerns have been raised about the long-term accumulating effects of triclocarban, a polychlorinated diarylurea widely used as an antibacterial soap additive, in the environment and in human beings. Indeed, the Food and Drug Administration has recently banned it from personal care products. Herein, we report the synthesis, antibacterial activity and cytotoxicity of novel N,N'-diarylureas as triclocarban analogs, designed by reducing one or more chlorine atoms of the former and/or replacing them by the novel pentafluorosulfanyl group, a new bioisostere of the trifluoromethyl group, with growing importance in drug discovery. Interestingly, some of these pentafluorosulfanyl-bearing ureas exhibited high potency, broad spectrum of antimicrobial activity against Gram-positive bacterial pathogens, and high selectivity index, while displaying a lower spontaneous mutation frequency than triclocarban. Some lines of evidence suggest a bactericidal mode of action for this family of compounds. Keywords: antibacterial; Gram-positive; N,N0-diarylureas; pentafluorosulfanyl; Staphylococcus aureus; triclocarban |
Note: | Reproducció del document publicat a: https://doi.org/10.3390/molecules23112853 |
It is part of: | Molecules, 2018, vol. 23, num. 11, p. 2853 |
URI: | http://hdl.handle.net/2445/128774 |
Related resource: | https://doi.org/10.3390/molecules23112853 |
ISSN: | 1420-3049 |
Appears in Collections: | Articles publicats en revistes (Institut de Biomedicina (IBUB)) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
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