475209-02-0Relevant academic research and scientific papers
Structural optimization and neurotrophic activity evaluation of neurotrophic gentiside derivatives
Wang, Zhenkang,Ma, Chunhua,Wang, Yujie,Xiao, Qiang,Xu, Chenghui,Li, Yingxia
, (2019/10/14)
C14 alkyl benzoate ABG001, derived from naturally occurring gentisides, was reported to exhibit neurotrophic activity which is similar to NGF (Nerve Growth Factor). In this research, ABG001 was modified by the strategy of isosteric replacement and conformational restriction with the purpose of improving the bioactivity. The cellular neurotrophic activity of those ABG001 derivatives were evaluated, among which 3-hydroxyquinolin-2-(1H)-one A3 and 4-decylphenol ester B7 displayed much better neurotrophic activity compared with ABG001, which highlights the potential of those novel scaffolds for future neurotrophic agent development.
Potential for minimal self-replicating systems in a dynamic combinatorial library of equilibrating imines
Morrow, Sarah M.,Bissette, Andrew J.,Fletcher, Stephen P.
, p. 5005 - 5010 (2017/07/27)
The presence of a self-replicator in a dynamic combinatorial library (DCL) offers function above and beyond libraries under thermodynamic control, moving towards out-of-equilibrium systems which mimic biological networks. In this work, we examine a previously reported DCL based on reversible imine formation to give amphiphilic structures. The amphiphilic imines were readily produced in organic solvents, and were found to aggregate to micelles in water as judged by diffusion-ordered NMR spectroscopy, dynamic light scattering and interferometric scattering microscopy. Unfortunately, the autocatalytic formation of products was not observed in water, and preformed imines slowly hydrolysed to aldehyde and amine components at neutral pD.
Alkyl phenylcarbinol polyoxyethylene ether and preparation method thereof
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Paragraph 0026, (2017/01/26)
The application discloses an alkyl phenylcarbinol polyoxyethylene ether and a preparation method thereof, the molecular structure of the alkyl phenylcarbinol polyoxyethylene ether comprises a hydrophobic group and a hydrophilic group, the molecular structural formula is shown in the description, wherein R in the molecular formula is alkyl, and n is equal to 3-50. The alkyl phenylcarbinol polyoxyethylene ether has excellent effects of moisturizing, permeating, emulsifying, dispersing, solubilizing and washing, can be used as an emulgator, a textile assistant, a detergent, a dispersing agent, a softening agent, a petroleum demulsifier and the like, completely replaces an alkylphenol ethoxylates emulgator, and is widely applied to the industries of detergents, personal care products, textile, paper-making, petroleum, pesticides, pharmacy, printing, synthetic rubbers, waterborne emulsions, coatings, printing ink, adhesives, plastics and the like.
Novel dicarboxylic acid derivatives
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Page/Page column 17, (2008/06/13)
The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.
Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships
Koide, Yuuki,Hasegawa, Takeshi,Takahashi, Atsuo,Endo, Akira,Mochizuki, Naoki,Nakagawa, Masako,Nishida, Atsushi
, p. 4629 - 4638 (2007/10/03)
Sphingosine-1-phosphate (S1P) is an intracellular second messenger and an extracellular mediator through endothelial differentiation gene (EDG) receptors, which are a novel class of G-protein-coupled receptors. Although EDG has attracted much attention because of its various roles, no selective agonists or antagonists have yet been developed. This could account for the delay in clarifying the physiological roles of members of the EDG family. Because precise structural information on EDG receptors is not yet available, pharmacophore models were generated based on structural information for S1P using the rational drug design software Catalyst. Novel antagonists, 2-alkylthiazolidine-4-carboxylic acids, were retrieved from a three-dimensional database search using the pharmacophore models, and these showed activity for EDG3. On the basis of their nonphosphoric acid structure, more potent antagonists, 2-(m- or p-heptylphenyl)thiazolidine-4-carboxylic acid, were developed.
Synthesis and immunosuppressive activity of 2-substituted 2- aminopropane-1,3-diols and 2-aminoethanols
Kiuchi, Masatoshi,Adachi, Kunitomo,Kohara, Toshiyuki,Minoguchi, Masanori,Hanano, Tokushi,Aoki, Yoshiyuki,Mishina, Tadashi,Arita, Masafumi,Nakao, Noriyoshi,Ohtsuki, Makio,Hoshino, Yukio,Teshima, Koji,Chiba, Kenji,Sasaki, Shigeo,Fujita, Tetsuro
, p. 2946 - 2961 (2007/10/03)
A series of 2-substituted 2-aminopropane-1,3-diols was synthesized and evaluated for their lymphocyte-decreasing effect and immunosuppressive effect on rat skin allograft. A phenyl ring was introduced into the alkyl chain of the lead compound 3, which is an immunosuppressive agent structurally simplified from myriocin (1, ISP-I) via compound 2. The potency of the various compounds was dependent upon the position of the phenyl ring within the alkyl side chain. The most suitable length between the quaternary carbon atom and the phenyl ring was two carbon atoms. 2-Substituted 2-aminoethanols were successively synthesized and evaluated for their T-cell-decreasing effect and immunosuppressive effect using a popliteal lymph node gain assay in rats. The absolute configuration at the quaternary carbon affected the activity, and the (pro-S)-hydroxymethyl group of compound 6 was essential for potent immunosuppressive activity. Favorable substituents for the (pro-R)- hydroxymethyl group of 6 were hydroxyalkyl (hydroxyethyl and hydroxypropyl) or lower alkyl (methyl and ethyl) groups. 2-Amino-2-[2-(4- octylphenyl)ethyl]propane-1,3-diol hydrochloride (6, FTY720) was found to possess considerable activity and is expected to be useful as an immunosuppressive drug for organ transplantation.
The Properties of Liquid Crystal Materials Incorporating the -CH2O- Inter-ring Linkage
Carr, N.,Gray, G. W.
, p. 27 - 44 (2007/10/02)
To establish more securely the influence of the -CH2O- inter-ring linkage upon the properties of mesogens of both high and low dielectric anisotropy, a range of ethers with the following general structure has been prepared and their properties examined. The thermal and electro-optic properties of the compounds are discussed, and comparisons made where possible with analogous materials incorporating the -CH2CH2- linkage.
