Onyedibe, Kenneth I. published the artcileSF5- and SCF3-substituted tetrahydroquinoline compounds as potent bactericidal agents against multidrug-resistant persister Gram-positive bacteria, SDS of cas: 1885-29-6, the main research area is pentafluorosulfanyl trifluoromethylthio substituted tetrahydroquinoline multidrug resistance; gram pos bacteria persister bactericidal agent.
Bacteria persister cells are immune to most antibiotics and hence compounds that are active against persister bacteria are needed. We screened a chem. library of SF5- and SCF3-substituted tetrahydroquinoline compounds, synthesized via the Povarov reaction, for antibacterial activity and identified active compounds that displayed good activities against many Gram-pos. bacteria, including persisters. The most potent of these compounds, HSD1835, inhibited the growth of drug-resistant Gram-pos. bacterial pathogens (including clin. strains) at concentrations ranging from 1 μg mL-1 to 4 μg mL-1. Several of the SCF3- and SF5-containing compounds were active against methicillin-resistant Staphylococcus aureus (MRSA) and against the two most fatal strains of vancomycin-resistant Enterococcus (VRE), VRE faecalis and VRE faecium. The compounds showed bactericidal activity against stationary phase persister MRSA in time-kill assays. Mechanistic studies showed that HSD1835 acts by disrupting bacterial membranes. SEM (SEM) was used to confirm bacterial membrane disruption. Interestingly, in a 30 day serial exposure experiment, MRSA remained susceptible to low-dose HSD1835 while resistance to ciprofloxacin and mupirocin emerged by day 10. Analogs of HSD1835, which did not bear the SF5 or SCF3 moieties, were inactive against bacteria. Recent reports (G.A.Naclerio, N.S.Abutaleb, K.I.Onyedibe, M.N.Seleem and H.O.Sintim, RSC Med.Chem. 2020, 11, 102-110 and G.A.Naclerio, N.S.Abutaleb, D.Li, M.N.Seleem and H.O.Sintim, J.Med.Chem. 2020, 63(20), 11934-11944) also demonstrated that adding the SF5 or SCF3 groups to a different scaffold (oxadiazoles) enhanced the antibacterial properties of the compounds, so it appears that these groups are privileged moieties that enhance the antimicrobial activities of compounds Naclerio, N. S. Abutaleb, D. Li, M. N. Seleem and H. O. Sintim, J. Med. Chem. 2020, 63(20), (11934-11944) also demonstrated that adding the SF5 or SCF3 groups to a different scaffold (oxadiazoles) enhanced the antibacterial properties of the compounds, so it appears that these groups are privileged moieties that enhance the antimicrobial activities of compounds
RSC Medicinal Chemistry published new progress about Antibacterial agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, SDS of cas: 1885-29-6.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts