Liuhong Yun's research while affiliated with Government of the People's Republic of China and other places
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Publications (11)
Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof.
The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compoun...
Introduction
Naturally occurring CD4+CD25+ regulatory T (Treg) cells are central to the maintenance of peripheral tolerance. Impaired activity and/or a lower frequency of these cells lead to systemic lupus erythematosus (SLE). Manipulating the number or activity of Treg cells is to be a promising strategy in treating it and other autoimmune disease...
For Abstract see ChemInform Abstract in Full Text.
The four amino-substituted β-cyclodextrins were synthesized and used as the chiral ligands to form the copper(II) complexes, respectively. CDen copper(II) complex was applied as the model selector to optimize the electrophoresis conditions and all the selected chiral dansyl amino acids were baseline separated under the proposed method, the optimum...
A novel class of chiral melamine derivatives has been designed and synthesized. The ability of these compounds to perform chiral recognition toward 19 natural chiral alpha-amino acids has been investigated by electrospray ionization tandem mass spectrometry for the first time. The enantioselectivities of these new chiral selectors are encouraging....
6(A)-(2-Aminoethylamino)-6(A)-deoxy-beta-cyclodextrin (CDen) was synthesized and formed a binary complex with Cu(II) which was shown to be an effective chiral selector for separation of underivatized amino acid enantiomers in capillary electrophoresis (CE). Moreover, the chiral resolution was greatly enhanced by the presence of polyethyl glycol (PE...
Iptakalim hydrochloride (N-(1-methylethyl)-1,1,2-trimethyl-propylamine hydrochloride) is a promising antihypertensive drug discovered and developed by Beijing Institute of Pharmacology and Toxicology. Deuterium- and tritium-labelled compounds were designed and synthesized for pharmacokinetic and pharmacological mechanism studies. A derivatization m...
Two types of lead structures for selective agonists of ETA, a biological target not yet fully elucidated, has first been discovered via diversity-guided pharmacophore simplification and simulation. And it is first demonstrated that potent selective ETA agonists might be useful for protection of endothelium and for prophylaxis and treatment of cardi...
It has been found that a Mannich-type reaction catalyzed by an intramolecular phenolic hydroxy group involves simply heating a hydroxybenzaldehyde with a secondary amine and a dialkyl phosphite in alcohol, produced highly substituted α-aminomethylphosphonates. The corresponding reaction can hardly be detected if the hydoxy group of the benzaldehyde...
A new highly efficient synthetic technology of microwave-promoted nucleophilic substitution of aryl chloride with amines is described. N-Alkyl-o-nitroaniline derivatives serving as building blocks can be rapidly synthesized in 50%-quantitive yields under microwave irradiation.
A γ-hydroxyphosphonate P6 (O1-methyl-O2-(1, 2, 2-trimethylpropyl)-2-hydroxy-5-nitrophenyl methylphosphonic acid) which is proposed to be an analog of the transition
state in hydrolysis of soman was synthesized. Artificial antigens were obtained by conjugating P6 to the carrier proteins BSA (bovine serum albumin) and LPH(Limulus polyphenus hemocyani...
Citations
... 37 The same group showed that in the same model, Foxp3 + RORct + Tregs ('biTregs') were pathogenic, at least in part, because RORct induce the secretion of IL-17 in biTreg cells. 38 A number of treatments in several murine models of lupus have been associated with increased Treg number or function, including, in MRL/lpr strain, IL-33 inhibition, piperlongumine and the 4hydroxyquinoline-3-formamide derivative (known as Y27) [39][40][41] ; in NZBxW/F1 mice, IL-2/IL-2 mAb immune complexes, G-CSF and tuftsin-phosphorylcholine [42][43][44] ; and in the bm12?B6 chronic graftversus-host model of lupus nephritis, microRNA-21 deficiency. 45 Progesterone may also be important for optimal Treg number and function, as progesterone-deficient Nba2 mice have increased antichromatin IgG and proteinuria associated with a decrease in Tregs. ...
Reference: Regulatory T cells in renal disease
... Amongst the selected mAbs against hapten (3b), one, PAR 15, displayed a noticeable catalytic activity (k cat /K m = 0.36 M À1 min À1 , (k cat /K m )/k uncat = 14,400 M À1 ). A few years latter, Wang and Yang used hapten (4) [36] and (5) [8,37], to select mAbs aimed at soman hydrolysis. Both allowed the selection of catalytically active mAbs. ...
... Dns-DL DL-AA [60] Trends Trends in Analytical Chemistry, Vol. 32, 2012 formation of ternary metal complexes with the analytes induces fine tuning of the separation, realizing selectivity hardly achievable otherwise. ...
... As shown in Figure 2, it appeared that some of the new synthesized chalcone derivatives (compounds 6c, 6d, 7a and 7b) exhibited 5-10 folds inhibitory activities against AChE than relative Flavokawain B Mannich base derivatives which were reported in our previous investigation. For the modification or optimization of flavokawain B Mannich base derivatives, structure simplification was employed, which was a widely used method in the drug discovery and development [19][20][21] . This method is benefit for the screening for pharmacophore or important structure domain in natural products, enhancing bioactivity or attenuating side effects. ...
... For an indirect enantioseparation, a selector is usually also necessary to resolve the derivatives. Selectors that are suitable for direct and indirect enantioseparation include cyclodextrins (CD) [12][13][14], crown ethers [15][16][17], macrocyclic antibiotics [18][19][20], chiral surfactants [21,22] and ligand-exchange complexes [23][24][25][26]. ...
... By now, different approaches, including circular dichroism (CD), nuclear magnetic resonance (NMR), and liquid chromatography (LC) have been widely applied into the field [2][3][4][5][6]. Due to its great performance in speed, sensitivity, and specificity, mass spectrometry (MS) has attracted much interest in the past 20 years in chiral analysis [3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18]. There are two basic points in MSbased chiral analysis experiments. ...