2766-42-9Relevant academic research and scientific papers
A γ-lactam siderophore antibiotic effective against multidrug-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter spp.
Goldberg, Joel A.,Kumar, Vijay,Spencer, Elizabeth J.,Hoyer, Denton,Marshall, Steven H.,Hujer, Andrea M.,Hujer, Kristine M.,Bethel, Christopher R.,Papp-Wallace, Krisztina M.,Perez, Federico,Jacobs, Michael R.,van Duin, David,Kreiswirth, Barry N.,van den Akker, Focco,Plummer, Mark S.,Bonomo, Robert A.
, (2021)
Serious infections caused by multidrug-resistant (MDR) organisms (Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii) present a critical need for innovative drug development. Herein, we describe the preclinical evaluation of YU253911,
Method for synthesizing benserazide hydrochloride by utilizing fixed bed hydrogenation equipment
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Paragraph 0028; 0034-0035, (2021/06/02)
The invention discloses a method for synthesizing benserazide hydrochloride by using fixed bed hydrogenation equipment, which is characterized in that a compound 1 reacts with an amino protective agent to carry out an amino protection reaction, so that the subsequent purification is easy, and the dosage of hydrazine hydrate in the synthesis method is small; according to the method, fixed bed hydrogenation equipment is used for synthesis, a fixed bed reactor is filled with a solid catalyst or a solid to realize a heterogeneous reaction process, the catalyst in the fixed bed reactor is relatively fixed, a reaction liquid flows through a bed layer, and the reaction liquid flows through the bed layer by adjusting the flow rate and the reaction pressure; qualified products can be obtained after reaction liquid flows out of the fixed bed, continuous production can be achieved, product deterioration caused by long-time contact of the products and the catalyst can be avoided, the same amount of products can be produced due to continuous production, the reactor size can be very small, the safety problem caused by high-pressure reaction is greatly reduced, the amount of the catalyst used in the reaction is less, and the production cost is reduced.
SIDEROPHORE CONJUGATED PYRAZOLIDINONES, AND ANALOGUES THEREOF
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Page/Page column 21, (2020/02/14)
In one aspect, the invention provides compounds and methods that are useful for treating bacterial infections.
A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli
Goldberg, Joel A.,Nguyen, Ha,Kumar, Vijay,Spencer, Elizabeth J.,Hoyer, Denton,Marshall, Emma K.,Cmolik, Anna,O'Shea, Margaret,Marshall, Steven H.,Hujer, Andrea M.,Hujer, Kristine M.,Rudin, Susan D.,Domitrovic, T. Nicholas,Bethel, Christopher R.,Papp-Wallace, Krisztina M.,Logan, Latania K.,Perez, Federico,Jacobs, Michael R.,Van Duin, David,Kreiswirth, Barry M.,Bonomo, Robert A.,Plummer, Mark S.,Van Den Akker, Focco
, p. 5990 - 6002 (2020/07/10)
Treatment of multidrug-resistant Gram-negative bacterial pathogens represents a critical clinical need. Here, we report a novel γ-lactam pyrazolidinone that targets penicillin-binding proteins (PBPs) and incorporates a siderophore moiety to facilitate uptake into the periplasm. The MIC values of γ-lactam YU253434, 1, are reported along with the finding that 1 is resistant to hydrolysis by all four classes of β-lactamases. The druglike characteristics and mouse PK data are described along with the X-ray crystal structure of 1 binding to its target PBP3.
Synthesis method of benserazide hydrochloride
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Paragraph 0126; 0127; 0130; 0131, (2019/12/11)
The invention relates to a synthesis method of benserazide hydrochloride. According to the synthesis method, serine methyl ester hydrochloride is taken as the primary raw material, at first, amino protection reactions are carried out; and then amine-ester exchange reactions, condensation reactions, reduction reactions, and de-protection reactions are performed to obtain high purity benserazide hydrochloride. The synthesis method has the advantages that the raw materials are cheap and easily available, the operation is convenient, the product purity and yield of each step are high, and thus thesynthesis method is suitable for industrial production.
Amino Acid Functionalized Organotin Trichlorides and Their Tin Sulfide Clusters
Engel, Annikka,Dehnen, Stefanie
, (2019/08/02)
We present a new synthesis of functionalized tin sulfide clusters via organotin trichlorides with boc-protected amino acids (RAAcSnCl3). In this work we used non-polar (alanine, valine, leucine, phenylalanine and methionine), polar/neutral (serine and tyrosine) and basic (histidine) amino acids. We obtained single crystals from a Boc-protected valine derivative of the originally used organotin trichloride R1SnCl3 [R1 = CMe2CH2C(O)Me] and determined its structure by means of X-ray diffraction. A subsequent reaction with sulfide sources led to a variety of respective cluster structures. By using either (Me3Si)2S or Na2S, the reaction product turns out to be the defect-heterocubane cluster [(RAAcSn)3S4Cl] or the “doppeldecker”-type cluster [(RAAcSn)4S6], respectively, according to 119Sn NMR spectroscopy.
A new synthesis of chiral oxazolidinones from the amino acid L-serine
Nogueira, Thais C. M.,Pinheiro, Alessandra C.,Kaiser, Carlos R.,Wardell, James L.,Wardell, Solange M. S. V.,De Souza, Marcus V. N.
, p. 626 - 631 (2013/12/04)
Cyclization of the (4S)-PhCH2OCONHCH(CH2OH)CONHN=CH- aryl, obtained in 4 steps from L-serine, on treatment with MeI and potassium carbonate, generates the chiral oxazolidinones, (4S)-N'-[(E)-(phenyl) methylidene]-Nmethyl- 2-oxo-1,3-o
