69350-76-1Relevant academic research and scientific papers
Application of nicotinamide riboside aromatic formate compound and composition thereof and compound crystal form
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, (2022/02/24)
The invention provides application of a nicotinamide riboside triaryl formate compound and a composition thereof in improving the level of coenzyme I (NAD) in the human body, improving health conditions or treating related diseases, and a compound in a crystal form shown in the formula (II-1). The structure of the nicotinamide riboside triaryl formate compound is as shown in a formula (I). As a synthesis precursor of NAD, compared with nicotinamide nucleoside, the nicotinamide nucleoside triaryl formate compound not only can effectively improve the level of NAD in the human body, but also is easier to prepare, the cost is remarkably reduced, and the nicotinamide nucleoside triaryl formate compound has remarkable industrial application advantages.
Substituted pyrazole compound, preparation method, pharmaceutical composition and applications thereof
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Paragraph 0378; 0383-0385, (2020/03/12)
The invention discloses a substituted pyrazole compound represented by a formula I, and a preparation method, a pharmaceutical composition and applications thereof, wherein the compound has characteristics of good stability, excellent solubility, low cytotoxicity and remarkable neuroprotective effect, can effectively prevent and treat nerve cell injury, and is an ideal medicinal compound for preventing or treating cerebral stroke, cerebral embolism, cerebral stroke sequelae, cerebral stroke dyskinesia, mitochondrial encephalomyopathy and amyotrophic lateral sclerosis of spinal cord.
3-Trifluoromethylpyrazolones derived nucleosides: Synthesis and antiviral evaluation
Ahmed, Ayman M. S.,Abou-Elkhair, Reham A. I.,El-Torky, Alaa M.,Hassan, Abdalla E. A.
, p. 590 - 603 (2019/04/03)
Dengue (DENV) viral infection is a global public health problem that infrequently develops life threatening diseases such as dengue hemorrhagic fever (DFS) and dengue shock syndrome (DSS). Middle East respiratory syndrome coronavirus (MERS-CoV) is a highly pathogenic human corona virus with 38% fatality rate of infected patients. A series of 4-arylhydrazono-5-trifluoromethyl-pyrazolones, their ribofuranosyl, and 5′-deoxyribofuranosyl nucleosides were synthesized, geometry optimized using Density functional theory (DFT), and evaluated for their antiviral activity. 2-Nitrophenylhydrazonopyra-zolone derivative 5 showed significant activity against MERS-CoV (EC50 = 4.6 μM). The nucleoside analog 8 showed moderate activity against DENV-2 (EC50 = 10 μM), while the activity was abolished with the corresponding 5′-deoxyribonucleoside analogs. The identified hits in this study set this category of compounds for further future optimizations.
Larger laboratory scale synthesis of 5-methyluridine and formal synthesis of its L-enantiomer
Thiesen, Luciano J. Hoeltgebaum,Cabral, Nadia,Joselice E Silva, Maria,Bezerra, Gilson,Doboszewski, Bogdan
, p. 249 - 264 (2017/06/19)
A larger laboratory scale synthesis (>60 g per run) of 5-methyluridine is presented. The critical intermediate 1,2-O-isopropylidene-α-D-ribofuranose was prepared from very cheap D-glucose via D-allose. Its L-enantiomer was obtained from L-arabinose via L-glucose, and also from L-xylose. {figure presented}.
Preparation of the tri-arabino di-mycolate fragment of mycobacterial arabinogalactan from defined synthetic mycolic acids
Mohammed, Mohsin O.,Al Dulayymi, Juma'a R.,Baird, Mark S.
supporting information, p. 36 - 42 (2016/11/25)
An efficient synthetic approach to tri-arabino di-mycolates, using structurally defined synthetic α-, keto and methoxy mycolic acids is described.
Gold(III)-catalyzed glycosidations for 1,2- trans and 1,2- cis furanosides
Thadke, Shivaji A.,Mishra, Bijoyananda,Hotha, Srinivas
, p. 7358 - 7371 (2014/09/29)
Stereoselective synthesis of furanosides is still a daunting task, unlike the pyranosides, for which several methods exist. Herein, a unified stereoselective strategy for the synthesis of 1,2-trans and 1,2-cis furanosides is revealed for seven out of eight possible isomers of pentoses. The identified protocol gives access to diastereoselective synthesis of α- and β-araf, ribf, lyxf, and α-xylf furanosides. 1,2-trans glycosides were synthesized by the use of propargyl 1,2-orthoesters under gold-catalyzed glycosidation conditions, and subsequently, they are converted into 1,2-cis glycosides through oxidation-reduction as the key functional group transformation. All the reactions are found to be fully diastereoselective, mild, and high yielding.
Facile synthesis of β- And α-arabinofuranosides and application to cell wall motifs of M. tuberculosis
Thadke, Shivaji A.,Mishra, Bijoyananda,Hotha, Srinivas
supporting information, p. 2466 - 2469 (2013/06/27)
Propargyl 1,2-orthoesters of arabinose are exploited for the synthesis of 1,2-trans furanosides; easily accessible 1,2-trans ribofuranosides are converted to challenging 1,2-cis-arabinofuranosides by oxidoreduction. Utility of these protocols was demonstrated by the successful synthesis of major structural motifs present in the cell surface of Mycobacterium tuberculosis. Key furanosylations were carried out under gold-catalyzed glycosidation conditions.
Automated solid phase synthesis of oligoarabinofuranosides
Kandasamy, Jeyakumar,Hurevich, Mattan,Seeberger, Peter H.
supporting information, p. 4453 - 4455 (2013/06/26)
Automated solid phase synthesis enables rapid access to the linear and branched arabinofuranoside oligosaccharides. A simple purification step is sufficient to provide the conjugation ready oligosaccharides in good yield.
Ready preparation of furanosyl n-pentenyl orthoesters from corresponding methyl furanosides
Ramamurty, Changalvala V. S.,Ganney, Parimala,Rao, C. Srinivas,Fraser-Reid, Bert
, p. 2245 - 2247 (2011/05/17)
The 3,5-di-O-benzoyl n-pentenyl orthoesters of the four pentofuranoses have been prepared. The first key intermediate in each case is the methyl pentofuranoside(s), and a user-friendly procedure for the preparation of each, based on the Callam-Lowary precedent, is described, whereby formation of the crucial α/β anomeric mixture is optimized. The mixture is used directly to prepare the corresponding perbenzoylated pentofuranosyl bromide(s) and then the title compounds.
2'-FLUORO-4'-SUBSTITUTED NUCLEOSIDES, THE PREPARATION AND USE
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Page/Page column 11, (2010/05/13)
The present invention provides 2'-fluorine-4'-substituted-nucleoside analogues or their pro-drugs or 5'-phosphate esters (including the pro-drugs of the 5'-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows: wherein: R = CH3, CH, N3, C≡CH; R' = H, F; X = F, OH, NH2; Y = H, CH3, F, OH, NH2 The compounds are used in the synthesis of drugs for the treatment of virus infection, especially for the treatment of HBV, HCV or HIV infection.
