94347-44-1Relevant articles and documents
Substrate-Inspired Fragment Merging and Growing Affords Efficacious LasB Inhibitors
Kaya, Cansu,Walter, Isabell,Yahiaoui, Samir,Sikandar, Asfandyar,Alhayek, Alaa,Konstantinovi?, Jelena,Kany, Andreas M.,Haupenthal, J?rg,K?hnke, Jesko,Hartmann, Rolf W.,Hirsch, Anna K. H.
supporting information, (2021/12/16)
Extracellular virulence factors have emerged as attractive targets in the current antimicrobial resistance crisis. The Gram-negative pathogen Pseudomonas aeruginosa secretes the virulence factor elastase B (LasB), which plays an important role in the infection process. Here, we report a sub-micromolar, non-peptidic, fragment-like inhibitor of LasB discovered by careful visual inspection of structural data. Inspired by the natural LasB substrate, the original fragment was successfully merged and grown. The optimized inhibitor is accessible via simple chemistry and retained selectivity with a substantial improvement in activity, which can be rationalized by the crystal structure of LasB in complex with the inhibitor. We also demonstrate an improved in vivo efficacy of the optimized hit in Galleria mellonella larvae, highlighting the significance of this class of compounds as promising drug candidates.
A Straightforward Homologation of Carbon Dioxide with Magnesium Carbenoids en Route to α-Halocarboxylic Acids
Monticelli, Serena,Urban, Ernst,Langer, Thierry,Holzer, Wolfgang,Pace, Vittorio
, p. 1001 - 1006 (2019/01/30)
The homologation of carbon dioxide with stable, (enantiopure) magnesium carbenoids constitutes a valuable method for preparing α-halo acid derivatives. The tactic features a high level of chemocontrol, thus enabling the synthesis of variously functionalized analogues. The flexibility to generate magnesium carbenoids through sulfoxide-, halogen- or proton- Mg exchange accounts for the wide scope of the reaction. (Figure presented.).
Preparation method of alpha-chloro carboxylic acid
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Paragraph 0056; 0057, (2018/04/26)
The invention discloses a preparation method of alpha-chloro carboxylic acid. According to the preparation method, amino acids are dissolved into hydrochloric acid to form a homogeneous solution; thenobtained homogeneous solution and a sodium nitrite water solution are simultaneously pumped into a mixing valve through an injection pump A and an injection pump B of a micro-channel reaction apparatus; after the solutions are fully mixed, the mixed solution is pumped into a micro reactor of the micro-channel reaction apparatus to carry out reactions at a constant flowing speed, and the flow-outliquid namely alpha-chloro carboxylic acid is collected. The provided method realizes the continuous production of alpha-chloro carboxylic acid; furthermore, the product quality is good, the operationis simple, the using amount of raw materials is little, the process is safe, the method is green and environmentally friendly, energy is saved, the efficiency is high, and thus the method is suitablefor industrial production.