159689-43-7Relevant academic research and scientific papers
Carbazole-based bis-ureas and thioureas as electroneutral anion transporters
Wang, Patrick,Wu, Xin,Gale, Philip A.
, p. 143 - 149 (2021)
We report a series of easily accessible carbazole-based bis-ureas and thioureas as effective anion receptors and transporters. The compounds exhibit moderate Cl? binding affinity in wet DMSO and Cl? transport capabilities in phospholipid membranes predominantly through an electroneutral H+/Cl? and anion exchange mechanisms.
Acridinone-based anion transporters
Gale, Philip A.,Macreadie, Lauren K.,Mcnaughton, Daniel A.
supporting information, p. 9659 - 9674 (2021/12/02)
The arrangement of hydrogen bond donors around a central lipophilic scaffold has proven to be a successful strategy in the development of potent chloride transporters. In this work, we revisit an acridinone 1,9-bis(thio)urea motif which had previously sho
HRI ACTIVATORS USEFUL FOR THE TREATMENT OF CARDIOMETABOLIC DISEASES
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Page/Page column 8-9, (2018/03/26)
New compounds of formula (I) are provided,wherein: X is CH or N, preferably CH; n is 1-5, preferably 1-2; m is 0-5, preferably 1-2; and, when m is 2-5, two of the R2 radicals taken together with two adjacent carbons of the benzene ring can form a 5- or 6-membered heterocyclic ring fused with the benzene ring. Compounds (I) are heme-regulated inhibitor (HRI) activators and useful for the prevention or treatment of cardiometabolic diseases such as metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus, non-alcoholic fatty liver disease, steatosis, non-alcoholic steatohepatitis, hypertension, dyslipidemia, atherosclerosis, and heart disease.
Pentafluorosulfanyl-containing triclocarban analogs with potent antimicrobial activity
Pujol, Eugènia,Blanco-Cabra, Núria,Julián, Esther,Leiva, Rosana,Torrents, Eduard,Vázquez, Santiago
supporting information, (2018/11/24)
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.
Synthesis of some arylsulfur pentafluoride pesticides and their relative activities compared to the trifluoromethyl analogues
Crowley, Patrick J.,Mitchell, Glynn,Salmon, Roger,Worthington, Paul A.
, p. 138 - 142 (2007/10/03)
Examples of pesticides containing an arylsulfur pentafluoride group were made and their biological activities compared to the corresponding trifluoromethyl analogues. A phenylsulfur pentafluoride analogue of the insecticide fipronil, screened against a resistant strain of Musca domestica, showed higher activity than the corresponding trifluoromethyl analogue.
