122350-80-5Relevant academic research and scientific papers
Alpha-galactosylceramide analogs, a preparation method thereof, and a pharmaceutical composition for treatment and prevention of diseases by abnormal immune modulation comprising the same
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Paragraph 0104-0108, (2019/07/10)
The present invention refers to alpha - ceramide analogs, including manufacturing method of immunomodulatory or pharmaceutical composition for treating or preventing diseases caused and relates to, more particularly NKT intracellular Th1 or selective activation reaction Th2 can be effective for treating or preventing diseases caused immunomodulatory or alpha - ceramide analogs, and manufacturing method of including a pharmaceutical composition for treating or preventing diseases caused immunomodulatory or more are disclosed. (by machine translation)
Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay
Lee, Sukjun,Lim, Donghyun,Lee, Eunyoung,Lee, Nakyung,Lee, Hong-Gun,Cechetto, Jonathan,Liuzzi, Michel,Freitas-Junior, Lucio H.,Song, Jin Sook,Bae, Myung Ae,Oh, Sangmi,Ayong, Lawrence,Park, Seung Bum
, p. 7425 - 7434 (2014/12/11)
New antimalarial agents that exhibit multistage activities against drug-resistant strains of malaria parasites represent good starting points for developing next-generation antimalarial therapies. To facilitate the progression of such agents into the development phase, we developed an image-based parasitological screening method for defining drug effects on different asexual life cycle stages of Plasmodium falciparum. High-throughput screening of a newly assembled diversity-oriented synthetic library using this approach led to the identification of carbohybrid-based 2-aminopyrimidine compounds with fast-acting growth inhibitory activities against three laboratory strains of multidrug-resistant P. falciparum. Our structure-activity relationship study led to the identification of two derivatives (8aA and 11aA) as the most promising antimalarial candidates (mean EC50of 0.130 and 0.096 μM against all three P. falciparum strains, selectivity indices >600, microsomal stabilities >80%, and mouse malaria ED50values of 0.32 and 0.12 mg/kg/day, respectively), targeting all major blood stages of multidrug-resistant P. falciparum parasites.
Synthesis of molecular frameworks containing two distinct heterocycles connected in a single molecule with enhanced three-dimensional shape diversity
Lim, Donghyun,Park, Seung Bum
supporting information, p. 7100 - 7108 (2013/06/27)
Herein, we report the synthesis of fused-triazole scaffolds that are connected by pyrimidines, pyrazoles, or pyrazolopyrimidines through carbohydrate-derived stereodivergent linkers. Pyrimidine-, pyrazole-, or pyrazolopyrimidine-based carbohybrids were co
Heteroaromatic moieties in the sphingosine backbone of α- Galactosylceramides for noncovalent interactions with CD1d
Kim, Yongju,Kim, Jonghoon,Oh, Keunhee,Lee, Dong-Sup,Park, Seung Bum
supporting information; experimental part, p. 151 - 154 (2012/04/04)
A series of α-GalCer analogues containing heterocyclic and aromatic moieties in the sphingosine backbone were synthesized to improve the selectivity in the Th1/Th2 cytokine profile via noncovalent interaction with three aromatic residues at the binding pocket of CD1d. In vitro and in vivo biological evaluations revealed the treatment of α-GalCer analogue (6) induced the selective stimulation of natural killer T cells to facilitate the secretion of Th2 cytokines.
Probing myo-inositol 1-phosphate synthase with multisubstrate adducts
Deranieh, Rania M.,Greenberg, Miriam L.,Le Calvez, Pierre-B.,Mooney, Maura C.,Migaud, Marie E.
supporting information, p. 9601 - 9619 (2013/01/16)
The synthesis of a series of carbohydrate-nucleotide hybrids, designed to be multisubstrate adducts mimicking myo-inositol 1-phosphate synthase first oxidative transition state, is reported. Their ability to inhibit the synthase has been assessed and resu
Regio- and stereoselectivity of the addition of O-, S-, N-, and C-nucleophiles to the β vinyl oxirane derived from D-glucal
Di Bussolo, Valeria,Caselli, Micaela,Romano, Maria Rosaria,Pineschi, Mauro,Crotti, Paolo
, p. 8702 - 8708 (2007/10/03)
6-O-Trityl- (1a) and 6-(O-benzyl)-substituted epoxide (1b) derived from D-glucal were examined in their addition reactions with O-, C-, N-, and S-nucleophiles. A 1,4-regio- and β-stereoselective or an anti 1,2-addition pathway is commonly observed dependi
New stereoselective beta-glycosylation via a vinyl oxirane derived from D-glucal.
Bussolo, Valeria Di,Caselli, Micaela,Pineschi, Mauro,Crotti, Paolo
, p. 3695 - 3698 (2007/10/03)
[reaction: see text] The reaction of the vinyl oxirane 1 derived from D-glucal with a series of O-nucleophiles (alcohols, phenol, and diacetone D-glucose) affords the corresponding 2-unsaturated beta-O-glycosides in a completely stereoselective way (syn 1
O-Alkylation at the anomeric centre for the stereoselective synthesis of Kdo-α-glycosides
Esswein, Angelika,Rembold, Hansjoerg,Schmidt, Richard R.
, p. 287 - 305 (2007/10/02)
O-Alkylation at the anomeric centre of the dianion of 4,5:7,8-di-O-cyclohexylidene-3-deoxy-N-methyl-α-D-manno-octulopyranosonamide (1) with several triflates led diastereoselectively to the α-glycosides.In this way, lipopolysaccharide building-blocks cont
