4627-61-6Relevant academic research and scientific papers
CHEMICAL UNCOUPLERS OF RESPIRATION AND METHODS OF USE THEREOF
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Paragraph 0246; 0249; 0259, (2020/11/27)
Uncoupling of respiration is a well-recognized process that increases respiration and heat production in cells. Provided herein are chemical uncouplers of respiration that are compounds of Formula (I). Also provided are methods for preventing or treating metabolic disorders and modulating metabolic processes using compound of Formula (I).
Cosmetic composition for eliminating or adsorbing particulate matter comprising peptide complex as effective component
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Paragraph 0031-0032; 0034-0046; 0063; 0065, (2020/03/17)
The present invention relates to a cosmetic composition for removing or adsorbing fine dust, containing a fatty acid-amino acid complex or a fatty acid-oligopeptide complex as an active ingredient. The complex of the present invention has an excellent effect of removing fine dust without skin toxicity, and thus can be effectively used as a composition for preventing or treating various diseases caused by fine dust.COPYRIGHT KIPO 2020
Organic compounds
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Page/Page column 22; 23; 33; 34, (2020/11/23)
A flavour composition comprising a compound according to the formula (I) or edible salts thereof, wherein R1 is an alkyl residue containing 6 to 20 carbon atoms, or an alkene residue containing from 9 to 25 carbon atoms with 1 to 6 double bonds, R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid, and NR2R3, in which R3 is H or together with R2 and the N-atom to which they are attached, a 5-membered ring, is a residue of an amino acid, in particular a proteinogenic amino acid, ornithine, gamma-aminobutyric acid or beta alanine, or a 1-amino cycloalkyl carboxylic acid.
Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 to Produce Analgesia in a Rat Model of Chronic Pain
Mostyn, Shannon N.,Rawling, Tristan,Mohammadi, Sarasa,Shimmon, Susan,Frangos, Zachary J.,Sarker, Subhodeep,Yousuf, Arsalan,Vetter, Irina,Ryan, Renae M.,Christie, Macdonald J.,Vandenberg, Robert J.
, p. 2466 - 2484 (2019/03/07)
Inhibitors that target the glycine transporter 2, GlyT2, show promise as analgesics, but may be limited by their toxicity through complete or irreversible binding. Acyl-glycine inhibitors, however, are selective for GlyT2 and have been shown to provide analgesia in animal models of pain with minimal side effects, but are comparatively weak GlyT2 inhibitors. Here, we modify the simple acyl-glycine by synthesizing lipid analogues with a range of amino acid head groups in both l- and d-configurations, to produce nanomolar affinity, selective GlyT2 inhibitors. The potent inhibitor oleoyl-d-lysine (33) is also resistant to degradation in both human and rat plasma and liver microsomes, and is rapidly absorbed following an intraperitoneal injection to rats and readily crosses the blood-brain barrier. We demonstrate that 33 provides greater analgesia at lower doses, and does not possess the severe side effects of the very slowly reversible GlyT2 inhibitor, ORG25543 (2).
Discovery of Hydrolysis-Resistant Isoindoline N -Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration
Lin, Hua,Long, Jonathan Z.,Roche, Alexander M.,Svensson, Katrin J.,Dou, Florence Y.,Chang, Mi Ra,Strutzenberg, Timothy,Ruiz, Claudia,Cameron, Michael D.,Novick, Scott J.,Berdan, Charles A.,Louie, Sharon M.,Nomura, Daniel K.,Spiegelman, Bruce M.,Griffin, Patrick R.,Kamenecka, Theodore M.
supporting information, p. 3224 - 3230 (2018/04/23)
N-Acyl amino acids directly bind mitochondria and function as endogenous uncouplers of UCP1-independent respiration. We found that administration of N-acyl amino acids to mice improves glucose homeostasis and increases energy expenditure, indicating that this pathway might be useful for treating obesity and associated disorders. We report the full account of the synthesis and mitochondrial uncoupling bioactivity of lipidated N-acyl amino acids and their unnatural analogues. Unsaturated fatty acid chains of medium length and neutral amino acid head groups are required for optimal uncoupling activity on mammalian cells. A class of unnatural N-acyl amino acid analogues, characterized by isoindoline-1-carboxylate head groups (37), were resistant to enzymatic degradation by PM20D1 and maintained uncoupling bioactivity in cells and in mice.
NOVEL GLYCINE TRANSPORT INHIBITORS FOR THE TREATMENT OF PAIN
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Page/Page column 78; 84, (2018/08/12)
The present invention relates to novel glycine transport inhibitor compounds and their use for treating pain.
Design and synthesis of lipids for the fabrication of functional lipidic cubic-phase biomaterials
Osornio, Yazmin M.,Uebelhart, Peter,Bosshard, Silvan,Konrad, Fabian,Siegel, Jay S.,Landau, Ehud M.
, p. 10583 - 10595 (2013/02/22)
A series of novel lipids with designed functionalities were synthesized. These lipids are based on conjugation of α-amino acids and their esters, cationic, anionic, neutral, and photochromic moieties to the lipophilic 9-cis octadecenyl chains by amide, ester, thioester, or amine bonds. Because of the plasticity of lipidic cubic phases, it is envisaged that when mixed with monooleoyl-rac-glycerol (monoolein, MO) and water at appropriate proportions, they would assemble to form bicontinuous lipidic cubic phases (LCPs) that exhibit the well-known material properties of LCPs such as phase stability, optical transparency, and chemical permeability. Moreover, due to the nature and position of the functionality at the headgroup region, we envision them to perform as functional materials by design.
