29107-83-3Relevant academic research and scientific papers
Design, synthesis, and evaluation of compounds capable of reducing Pseudomonas aeruginosa virulence
Hossain, Mohammad Anwar,Sattenapally, Narsimha,Parikh, Hardik I.,Li, Wei,Rumbaugh, Kendra P.,German, Nadezhda A.
, (2019/11/26)
Anti-virulence approaches in the treatment of Pseudomonas aeruginosa (PA)-induced infections have shown clinical potential in multiple in vitro and in vivo studies. However, development of these compounds is limited by several factors, including the lack of molecules capable of penetrating the membrane of gram-negative organisms. Here, we report the identification of novel structurally diverse compounds that inhibit PqsR and LasR-based signaling and diminish virulence factor production and biofilm growth in two clinically relevant strains of P. aeruginosa. It is the first report where potential anti-virulent agents were evaluated for inhibition of several virulence factors of PA. Finally, co-treatment with these inhibitors significantly reduced the production of virulence factors induced by the presence of sub-inhibitory levels of ciprofloxacin. Further, we have analyzed the drug-likeness profile of designed compounds using quantitative estimates of drug-likeness (QED) and confirmed their potential as hit molecules for further development.
One-pot synthesis of aryl sulfones from organometallic reagents and iodonium salts
Margraf, Natalie,Manolikakes, Georg
, p. 2582 - 2600 (2015/03/18)
A transition-metal-free arylation of lithium, magnesium, and zinc sulfinates with diaryliodonium salts is described. The sulfinic acid salts were prepared from the reaction of the corresponding organometallic reagents and sulfur dioxide. Combination of the three single steps (preparation of the organometallic compound, sulfinate formation, and arylation) leads to a one-pot sequence for the synthesis of aryl sulfones from simple starting materials. The chemoselectivity of unsymmetrical diaryliodonium salts has been investigated. Potential and limitations of this method will be discussed.
4-(Phenylsulfonyl)butanoic Acid. Preparation, Dianion Generation, and Application to Four-Carbon Chain Extension
Thompson, Charles M.,Frick, Jeffrey A.
, p. 890 - 896 (2007/10/02)
The bishomoenolate dianion of 4-(phenylsulfonyl)butanoic acid was investigated.It was observed the dianion could be generated in greater than 95percent yield with 200 mol percent of n-BuLi at certain concentrations.The dianion was reacted with a variety o
"REMOTE" DIANIONS-I. UTILITY OF 4-PHENYLSULFONYLBUTANOIC ACID IN THE MILD CONVERSION OF ALDEHYDES AND KETONES TO LACTONES.
Thompson, Charles M.
, p. 4243 - 4246 (2007/10/02)
Ketones and aldehydes are converted to lactones in high yield by stepwise treatment with the dianion of 4-phenylsulfonylbutanoic acid and trifluoroacetic anhydride.
