252580-08-8Relevant academic research and scientific papers
SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
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Paragraph 0633; 0364, (2015/06/10)
The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
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Page/Page column 107-108, (2014/12/12)
Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Ring-opening of oxazolines derived from l-serine: a short and efficient stereoselective synthesis of all four diastereomers of 3-mercaptoaspartic acid derivatives
Lee, Sang-Hyeup,Bok, Juhan,Qi, Xin,Kim, Sook Kyung,Lee, Yoon-Sik,Yoon, Juyoung
, p. 7309 - 7312 (2008/03/13)
Facile methods are described for accessing four diastereomerically pure 3-mercaptoaspartic acid derivative from l-aspartic acid. In our synthesis, ring-opening reactions of oxazoline-4,5-dicarboxylate with thiolacetic acid as well as the stereochemical interconversion of both α- and β-configuration via oxazoline chemistry were utilized as key steps.
An efficient approach to D-threo-3-hydroxyaspartic acid for the synthesis of novel L-threo-oxazolines as selective blockers of glutamate reversed uptake
De Angelis, Meri,Campiani, Giuseppe
, p. 2355 - 2357 (2007/10/03)
An efficient, stereoselective synthetic strategy to D-threo-3- hydroxyaspartic acid was developed. Starting from L-(2S,3S)-N-benzoyl-3- hydroxyaspartic acid dimethyl ester by a Deoxo-fluor-catalyzed cyclization reaction, an inversion of configuration at the β-center (erythro isomer), was observed. A base-induced epimerization reaction led to the D-trans-isomer, which was hydrolyzed to give D-threo-3-hydroxyaspartic acid with excellent stereoselectivity and overall yield. Starting from D-threo-3-hydroxyaspartic acid, L-threo-oxazolines can be stereoselectively synthesized.
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). New glutamate and aspartate analogues as potential neuroprotective agents
Campiani,De Angelis,Armaroli,Fattorusso,Catalanotti,Ramunno,Nacci,Novellino,Grewer,Ionescu,Rauen,Griffiths,Sinclair,Fumagalli,Mennini
, p. 2507 - 2510 (2007/10/03)
Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues 1a and 3 represent novel lead compounds f
A practical method for the synthesis of β-amino α-hydroxy acids. Synthesis of enantiomerically pure hydroxyaspartic acid and isoserine
Cardillo, Giuliana,Gentilucci, Luca,Tolomelli, Alessandra,Tomasini, Claudia
, p. 1727 - 1730 (2007/10/03)
The iodocyclization of 3-benzoylamino carboxylic acid derivatives gives oxazoline-5-carboxylates which are precursors of β-amino-α-hydroxy acids.
