127357-37-3Relevant academic research and scientific papers
The novel and efficient direct synthesis of N,O-acetal compounds using a hypervalent iodine(III) reagent: An improved synthetic method for a key intermediate of discorhabdins
Harayama, Yu,Yoshida, Masako,Kamimura, Daigo,Kita, Yasuyuki
, p. 1764 - 1766 (2005)
The use of hypervalent iodine(III) reagents allowed us to develop the novel and efficient direct synthesis of N,O-acetal compounds via the oxidative fragmentation reaction of α-amino acids or α-amino alcohols; furthermore, we succeeded in developing an im
Preparation method of Wittig-Horner reagent
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Paragraph 0030-0032; 0035-0037, (2021/07/31)
A preparation method of a Wittig-Horner reagent is disclosed. According to the preparation method of the Wittig-Horner reagent provided by the invention, a compound with a structure as shown in a formula (I) and a glyoxylic acid aqueous solution with a sp
Total Synthesis and Structure-Activity Relationships Study of Odilorhabdins, a New Class of Peptides Showing Potent Antibacterial Activity
Sarciaux, Matthieu,Pantel, Lucile,Midrier, Camille,Serri, Marine,Gerber, Cristelle,Marcia De Figueiredo, Renata,Campagne, Jean-Marc,Villain-Guillot, Philippe,Gualtieri, Maxime,Racine, Emilie
, p. 7814 - 7826 (2018/09/06)
The spread of antibiotic-resistant pathogens is a growing concern, and new families of antibacterials are desperately needed. Odilorhabdins are a new class of antibacterial compounds that bind to the bacterial ribosome and kill bacteria through inhibition
Reversible Folding of a β-Hairpin Peptide by a Metal-Chelating Amino Acid
Reutzel, Jan,Diogo, Timm M.,Geyer, Armin
supporting information, p. 8450 - 8456 (2017/06/28)
5-(1-Hydroxy-pyridin-2(1H)-onyl)-l-alanine (Hop) is a N-hydroxy-1,2-pyridone functionalized α-amino acid with the desired metal-chelating properties of DOPA (3,4-dihydroxy phenylalanine) but without its unwanted redox activity. The Fmoc-protected amino acid Fmoc-l-Hop(tBu)-OH (11) was synthesized from glycine phosphonate followed by enzymatic hydrolysis of the methyl ester yielding the Hop l-isomer in 96 % ee. The amino acid 11 is used in automated peptide synthesis for the assembly of a 14mer β-hairpin peptide with the sequence [dsb1, 14]H-CHXETGKHGHKLVC-OH (X=W, l-Hop). While the 10 π electron containing indole side chain of l-Trp in peptide 14 completes the formation of a hydrophobic cluster and results in 90 % folding, the folded fraction is significantly decreased to approximately 30 % for the 6 π electron l-Hop side chain in peptide 16. Metal chelation of Ga3+ reconstitutes the folding of 16 to above 60 % due to the formation of the Ga(16)3 trimer. The chelation process of 16 is monitored by NMR spectroscopy and the subsequent release of Ga3+ by a competitive metal chelator exemplifies the reversible oligomerization of peptide epitopes by metal chelation, bearing the opportunity to synthesize protein-sized aggregates on the basis of reversible chemistry in water.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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Paragraph 230, (2016/08/23)
The invention relates to novel heteroaryl and heterocycle compounds of formula I and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 109; 110, (2014/02/16)
The invention relates to novel heteroaryl and heterocycle compounds and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3k and for treating inflammatory and autoimmune disorders diseases and cancer.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITION AND METHODS THEREOF
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Page/Page column 136; 137, (2014/02/16)
Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 138, (2014/02/16)
Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune disorders diseases and cancer.
BARETTIN AND DERIVATIVES THEREOF FOR MEDICAL USE, IN PARTICULAR FOR THE TREATMENT OF DISEASES RELATED TO OXIDATIVE STRESS OR INFLAMMATION, AND FOR PRESERVING OR WASHING ORGANS
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Page/Page column 22, (2014/10/18)
The present invention relates to compounds of formula(I) herein, which includes barettin and derivatives thereof, or any pharmaceutically acceptable salt thereof for use as a medicament. Further the present invention relates to same compounds for use in t
SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS
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Page/Page column 109, (2013/09/26)
The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
