3696-28-4Relevant articles and documents
Biocatalytic synthesis of diaryl disulphides and their bio-evaluation as potent inhibitors of drug-resistant Staphylococcus aureus
Saima,Soni, Isha,Lavekar, Aditya G.,Shukla, Manjulika,Equbal, Danish,Sinha, Arun K.,Chopra, Sidharth
, p. 171 - 178 (2019/01/04)
Staphylococcus aureus is a WHO Priority II pathogen for its capability to cause acute to chronic infections and to resist antibiotics, thus severely impacting healthcare systems worldwide. In this context, it is urgently desired to discover novel molecules to thwart the continuing emergence of antimicrobial resistance. Disulphide containing small molecules has gained prominence as antibacterials. As their conventional synthesis requires tedious synthetic procedure and sometimes toxic reagents, a green and environmentally benign protocol for their synthesis has been developed through which a series of molecules were obtained and evaluated for antibacterial activity against ESKAPE pathogen panel. The hit compound was tested for cytotoxicity against Vero cells to determine its selectivity index and time-kill kinetics was determined. The activity of hit was determined against a panel of S. aureus multi-drug resistant clinical isolates. Also, its ability to synergize with FDA approved drugs was tested as was its ability to reduce biofilm. We identified bis(2-bromophenyl) disulphide (2t) as possessing equipotent antimicrobial activity against S. aureus including MRSA and VRSA strains. Further, 2t exhibited a selectivity index of 25 with concentration-dependent bactericidal activity, synergized with all drugs tested and significantly reduced preformed biofilm. Taken together, 2t exhibits all properties to be positioned as novel scaffold for anti-staphylococcal therapy.
Low-salt or salt-free microbicidal composition based on isothiazolone derivatives and pyrion disulphide
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Page/Page column 7, (2008/06/13)
The present invention relates to a low-salt or salt-free microbicidal preparation which comprises a) at least one fungicide selected from amongst isothiazolone derivatives and b) at least one stabilizer, where the at least one stabilizer is 2,2'-dithiobis(pyridine N-oxide). The microbicidal composition according to the invention is particularly suitable for the preservation of industrial products. The invention also relates to the use of 2,2'-dithiobis(pyridine N-oxide) as stabilizer in low-salt or salt-free isothiazolone-containing microbicidal preparations.
A facile preparation method for α,α-difluoroalkanecarboxylic acids and esters. A formal difluoromethylene insertion to alkanecarboxylic acids using radical reaction
Okano, Takashi,Takakura, Nobuyuki,Nakano, Yuko,Okajima, Asako,Eguchi, Shoji
, p. 1903 - 1920 (2007/10/02)
Various alkyl radicals generated by the photoreaction of a series of Barton esters reacted with 1,1-dichloro-2,2-difluoroethene to give radical adducts as the major product accompanied with self-trapping products. Primary, secondary, tertiary, benzyl, and some unsaturated alkyl radicals as well as those with another functional group such as ether, carbonyl, and azide were applicable. Barton esters of diacids also afford 1:2 adducts with a small amount of 1:1 adducts and bis-self-trapping products except for the succinic case. These adducts were hydrolyzed with AgNO3/H2O-THF to α,α-difluoroalkanecarboxylic acids and methanolyzed with AgNO3/MeOH to the corresponding methyl esters. 4-Azido-2,2-difluorobutylic acid and the methyl ester were converted to difluoro-GABA and difluoro-γ-lactams.
