2441-41-0Relevant articles and documents
HUMAN MICROBIOTA DERIVED N-ACYL AMIDES FOR THE TREATMENT OF HUMAN DISEASE
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Page/Page column 87-88, (2019/01/17)
The present invention provides compositions and methods for the modulation of G protein-coupled receptors (GPCRs). The invention provides a genetically engineered cell, wherein the cell expresses a human microbial N-acyl synthase (hm-NAS) gene. In one embodiment, the hm-NAS gene is N-acyl serinol synthase. The invention provides a probiotic composition, the probiotic composition comprises a genetically engineered cell of the invention. The invention provides a method for modulating a G protein-coupled receptor (GPCR) activity in a subject, the method comprises administering to the subject an effective amount of a composition comprising at least one selected from the group consisting of a genetically engineered cell, an hm-NAS gene, and a N-acyl amide.
Enzymic synthesis, physicochemical, and cell activity of glucosyl ester derivatives based on N-fatty acyl amino acid
An, Dong,Feng, Dexin
, p. 653 - 662 (2019/02/25)
Series of glucosyl esters derivatives were synthesized by enzymatic acylation and some surface properties, and cell activity were calculated and tested. The antitumor activity in vitro against three cancer cells, human colon carcinoma (K562), human hepatoma (HepG2), and human breast adenocarcinoma (MCF-7) of compounds, were evaluated using MTT methods. The glucosyl esters could significantly displayed high anticancer activity. Thereinto, compounds 12 and 12′ showed higher inhibition effect to cancer cells than others. Several compounds were more active than control drug 5-FU. The structure–activity relationship analysis revealed that lipophilic properties might be essential parameter for their activity.
Long-acting entecavir prodrug and preparation method and application thereof
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Paragraph 0081; 0082; 0084, (2019/04/17)
The invention relates to a long-acting entecavir prodrug and a preparation method and application thereof. The long-acting entecavir prodrug has a structure shown as formula I that is shown in the description; the long-acting entecavir prodrug can release slowly, continuously and stably in vivo and convert into an entecavir material technical, so that long acting is achieved. In the formula I, R1,R2 and R3 are defined the same as in the description.
Lipid dipeptide and gel
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Page/Page column 23-24, (2016/05/19)
A gelator that includes a lipid peptide of Formula (1) wherein R1 is a C9-23 aliphatic group, R2 is a hydrogen atom or a C1-4 alkyl group optionally having a C1-2 branched chain, R3 is a —(CH2)n—X group, n is a number from 1 to 4, and X is an amino group, a guanidino group, a —CONH2 group, or a 5-membered ring optionally having 1 to 3 nitrogen atoms, a 6-membered ring optionally having 1 to 3 nitrogen atoms, or a fused heterocycle including a 5-membered ring and a 6-membered ring that optionally has 1 to 3 nitrogen atoms; or a pharmaceutically usable salt of the lipid peptide.
Method for synthesizing fatty acyl glycocoll
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Paragraph 0027; 0028, (2017/01/02)
The invention discloses a method for synthesizing fatty acyl glycocoll. The method comprises the steps that an oxidant, a catalyst promoter and an alkali solution are mixed into an aqueous solution, the aqueous solution is added into an organic solvent system formed by mixing fatty acid monoethanolamide and a catalyst, a reaction is carried out for 0.5-3 h under the condition of maintaining the pH of the whole mixed system to be 6.0-12.0 and the temperature to be 20-40 DEG C, then a reaction is carried out for 0.5-2 h under stirring, and a product containing fatty acyl glycocoll is obtained. According to the method for synthesizing fatty acyl glycocoll, the reaction speed and the product yield are high, the reaction condition is mild and easy to control, and the method for synthesizing fatty acyl glycocoll is efficient, conforms to environment-friendly chemistry and is capable of facilitating industrialized production.
Enzymatic synthesis and characterization of galactosyl monoesters
An, Dong,Zhao, Xiaohui,Ye, Zhiwen
, p. 32 - 38 (2015/07/20)
Enzyme-catalyzed synthesis of several fatty acyl-amino acid esters based on d-galactose, as well as their chemical evaluation, was performed. These novel galactosyl fatty acyl-amino acid monoesters were synthesized by utilizing lipase from lipozyme TL IM in tert-butanol with d-galactose and fatty acyl-amino acids as starting materials. The products were characterized by 1H NMR, 13C NMR and MS analysis. In addition, their primary physical properties, such as hydrophilic-lipophilic balance (HLB), critical micellar concentration (CMC), solubility in water, maximum surface excess (Γmax), and minimal surface tension (Amin) were measured. The experimental results showed that their CMC values are between 5 and 0.4 mM. The HLB values of galactosyl esters 15-17 indicate that they are useful as oil-in-water emulsions or detergents, whereas 18-22 can be employed as water-in-oil emulsifiers or wetting agents.
Structure and thermotropic phase behavior of a homologous series of n -Acylglycines: Neuroactive and antinociceptive constituents of biomembranes
Reddy, S. Thirupathi,Krovi, Krishna Prasad,Swamy, Musti J.
, p. 4944 - 4954 (2014/12/10)
N-Acylglycines (NAGs) with different acyl chains have been found in the mammalian brain and other tissues. They exhibit significant biological and pharmacological properties and appear to play important roles in communication and signaling pathways within and between cells. In view of this, a homologous series of NAGs have been synthesized and characterized in the present study. Differential scanning calorimetric (DSC) studies show that the transition enthalpies and entropies of dry as well as hydrated NAGs exhibit a linear dependence on the acyl chain length. Most of the NAGs show a minor transition below the chain-melting phase transition, suggesting the presence of polymorphism in the solid state. Structures of N-myristoylglycine (NMG) and N-palmitoylglycine (NPG) were solved in monoclinic system with C2/c and P21 space groups, respectively. Analysis of the crystal structures show that NAGs are organized in a bilayer fashion, with head-to-head (and tail-to-tail) arrangement of molecules. The acyl chains in both structures are essentially perpendicular to the bilayer plane, which is consistent with a lack of odd-even alternation in the thermodynamic properties. The bilayer is stabilized by strong hydrogen bonding interactions between COOH groups of the molecules from opposite leaflets as well as N-H···O hydrogen bonds between the amide groups of adjacent molecules in the same leaflet and dispersion interactions among the acyl chains. Powder X-ray diffraction data show that the d-spacings for the NAGs with different acyl chains (n = 8-20) exhibit a linear dependence on the chain length, suggesting that all the NAGs investigated here adopt a similar packing arrangement in the crystal lattice. These observations are relevant for understanding the role of N-acylglycines in biological membranes.
N-Alkylamido-d-glucamine-based gelators for the generation of thixotropic gels
Ohsedo, Yutaka,Oono, Masashi,Saruhashi, Kowichiro,Watanabe, Hisayuki
, p. 48554 - 48558 (2014/12/10)
Hydrogels made from new gelators, composed of the alkyl chain and a d-glucamine moiety linked together with glycine(s), exhibit thixotropic properties, whereas the hydrogels formed with structurally similar N-alkyl-d-glucamide, which do not contain the glycine moiety, have a tendency to crystallize and do not show thixotropic behaviour.
The relationship between the structure and properties of amino acid surfactants based on glycine and serine
Qiao, Weihong,Qiao, Yangyang
, p. 821 - 828 (2013/11/06)
Two series of surfactants based on glycine and serine were synthesized with aproic acid, octanoic acid, decanoic acid, dodecanoic acid, tetradecanoic acid and hexadecanoic acid. All the surfactants were characterized by MS and 1H NMR, the structures of the synthesized surfactants are correct and the signals in MS and 1H NMR can be explained. The reaction conditions, surface properties and foam properties were studied. For the two series of surfactants, critical micelle concentration (CMC) and γ CMC (surface tension at CMC) decrease and surface activity is enhanced as the length of carbon chain increases. The surfactants with tetradecanoyl and hexadecanoyl groups show a good foaming property and especially, the long-chain acyl-serine performs better. These are all related to the hydromethyl group in the serine.
New N-acylamino acids and derivatives from renewable fatty acids: Gelation of hydrocarbons and thermal properties
Duarte, Rodrigo Da Costa,Ongaratto, Renata,Piovesan, Luciana Almeida,De Lima, Vania Rodrigues,Soldi, Valdir,Merlo, Aloir Ant?nio,D'Oca, Marcelo G. Montes
, p. 2454 - 2460 (2012/06/01)
This work reports the synthesis of new fatty N-acylamino acids and N-acylamino esters from the C16:0, C18:0, C18:1, and C18:1(OH) fatty acid families and demonstrates the activity of these compounds as organogel agents. Compounds were heated and dissolved in various solvents (n-hexane, toluene, and gasoline). Only saturated C16:0 and C18:0 derived from alanine were able to form gels in toluene, and saturated C16:0 derived from phenylalanine showed gelation in n-hexane. This is the first evidence that fatty N-acylamino esters and N-acylamino acid derivatives of l-serine and fatty acids C16:0, C18:0, and C18:1 are able to form gels with hexane. This observation confirms the importance of the hydroxyl group in the segment derivative of l-serine in forming good gels.
