5251-81-0Relevant academic research and scientific papers
Design of a "new motif" with β-amino acids and α-aminoxy acids: Synthesis of hybrid peptides with 12/10-helix
Sharma, Gangavaram V. M.,Manohar, Vennampalli,Dutta, Samit K.,Subash, Velaparthi,Kunwar, Ajit C.
, p. 3689 - 3698 (2008)
(Figure Presented) Hybrid peptides are prepared from a C-linked carbo-β-amino acid ester (R-β-Caa) and an α-aminoxy acid (R-Ama) derived from S-lactic acid. Extensive NMR (in CDCl3 solution), CD, and MD studies on the tetra- and hexapeptides led to identification of robust 12/10-mixed helices. The dipeptide repeat having an R-β-Caa and an R-Ama thus provides a "new motif" to realize a 12/10-mixed helix, for the first time, in oligomers containing R-Ama. To understand the impact of side chains in the mixed helix formation, R-β-Caa/Ama (with no substitution in Ama) and S-β-hAla/R-Ama oligomers were investigated. NMR studies revealed the existence of 12/10-helices in these hybrid peptides, and the side chains of monomers were found to have a profound influence on their stabilities. These observations imply that the propensity of β-amino acid to prefer a mixed 12/10-helix governs the structural behavior in these peptides. The structural consequences of the lone-pair repulsion between nitrogen and oxygen atoms result in a new and interesting structural motif which behaves like "pseudo" β3,β2-peptides in generating 12/10-mixed helices.
HYDROXAMATE COMPOUNDS AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR
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Paragraph 00548, (2021/01/23)
The present invention relates to compounds of formula I shown below: (I) wherein R1, R2 and R3 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.
Substituted benzimidazole compound and composition with compound
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Paragraph 0164-0169, (2019/03/31)
The invention provides a substituted benzimidazole compound and a composition with the compound. The substituted benzimidazole compound is a compound of formula (I) as shown in the specification, or apharmaceutically acceptable salt, prodrug, aquo-complex or solvent compound, polycrystalline type compound, stereisomer or isotope variant of the compound. The compound provided by the invention canbe adopted to treat and/or prevent related diseases caused by MEK (Methyl Ethyl Ketone), such as excessive proliferative diseases, pancreatitis, kidney illness, blastocyte cell transplantation and angiogenesis or angiopoiesis related diseases.
Rhodium-Catalyzed Cyclization of O,ω-Unsaturated Alkoxyamines: Formation of Oxygen-Containing Heterocycles
Escudero, Julien,Bellosta, Véronique,Cossy, Janine
supporting information, p. 574 - 578 (2018/02/21)
O,ω-Unsaturated N-tosyl alkoxyamines undergo unexpected RhIII-catalyzed intramolecular cyclization by oxyamination to produce oxygen-containing heterocycles. Mechanistic studies show that an aziridine intermediate seems to be responsible for the formation of the heterocycles, possibly via a RhV species.
Effect of optically active ethyl 2-phthalimidooxypropionate on the growth of cress, lepidium sativum
Takekida, Yukinori,Okazaki, Momotoshi,Shuto, Yoshihiro
, p. 1831 - 1833 (2007/10/03)
The effects of 2-phthalimidooxyalkanoic acid derivatives on the germination and root-growth of cress were examined. Since 2-phthalimidooxypropionates were most effective, the optically active ethyl esters were prepared. As the result of biological testing, the (S)-(+)-isomer exhibited stronger activity than the (R)-(+)-isomer. This result is contrary to those from commercial herbicides with similar structures, phenoxy- and oxyphenoxy-propionate-type compounds, where the (R)-isomers are generally known to be the active principles.
Synthesis and Anticonvulsant Activity of Imidooxy Derivatives
Edafiogho, Ivan O.,Scott, K. R.,Moore, Jacqueline A.,Farrar, Vida A.,Nicholson, Jesse M.
, p. 387 - 392 (2007/10/02)
Previous results of anticonvulsant activity in several imidooxy carboxylates related to (aminooxy)acetic acid in young chicks, prompted an in-depth reinvestigation of these analogues in mice.A series of 22 succinimidooxy, phthalimidooxy, and naphthalimido
ORGANIC SYNTHESES WITHOUT SOLVENT : PREPARATION OF ALKOXYPHTHALIMIDES AND OF ALKOXYLAMINES
Galons, Herve,Fiet, Jean,Combet-Farnoux, Claude,Miocque, Marcel,Bram, Georges
, p. 521 - 528 (2007/10/02)
Alkoxyphthalimides are prepared by alkylation of N-hydroxyphthalimide under solid-liquid phase transfer catalysis without solvent.When conversion of alkoxyphthalimides into alkoxylamines is nearly complete, neat hydrazine hydrate is added at room temperature.
