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Title: Pentafluorosulfanyl-containing Triclocarban Analogs with Potent Antimicrobial Activity
Author: Pujol, Eugènia
Blanco Cabra, Nuria
Julián, Esther
Leiva Martínez, Rosana
Torrents Serra, Eduard
Vázquez Cruz, Santiago
Keywords: Medicaments antibacterians
Citotoxicitat per mediació cel·lular
Disseny de medicaments
Síntesi orgànica
Antibacterial agents
Cell-mediated cytotoxicity
Drug design
Organic synthesis
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:
It is part of: Molecules, 2018, vol. 23, num. 11, p. 2853
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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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