50889-30-0Relevant academic research and scientific papers
Synthesis and pharmacological characterization of mitochondrial KATP channel openers with enhanced mitochondriotropic effects
Testai, Lara,Sestito, Simona,Martelli, Alma,Gorica, Era,Flori, Lorenzo,Calderone, Vincenzo,Rapposelli, Simona
, (2021)
Mitochondria play a key role for deciding fate of cells and thus are considered an attractive target for pharmacological interventions focused on containment of myocardial ischemia/reperfusion (I/R) injury. Notably, the activation of mitochondrial potassi
First Total Syntheses of Novel Non-Enzymatic Polyunsaturated Fatty Acid Metabolites and Their Identification in Edible Oils
Pavlí?ková, Tereza,Bultel-Poncé, Valérie,Guy, Alexandre,Rocher, Amandine,Reversat, Guillaume,Vigor, Claire,Durand, Thierry,Galano, Jean-Marie,Jahn, Ullrich,Oger, Camille
, p. 10090 - 10098 (2020)
Oxidative stress (OS) is an in vivo process leading to free radical overproduction, which triggers polyunsaturated fatty acid (PUFA) peroxidation resulting in the formation of racemic non-enzymatic oxygenated metabolites. As potential biomarkers of OS, their in vivo quantification is of great interest. However, since a large number of isomeric metabolites is formed in parallel, their quantification remains difficult without primary standards. Three new PUFA-metabolites, namely 18-F3t-isoprostane (IsoP) from eicosapentaenoic acid (EPA), 20-F4t-neuroprostane (NeuroP) from docosahexaenoic acid (DHA) and 20-F3t-NeuroP from docosapentaenoic acid (DPAn-3) were synthesized by two complementary synthetic strategies. The first one relied on a racemic approach to 18(RS)-18-F3t-IsoP using an oxidative radical anion cyclization as a key step, whereas the second used an enzymatic deracemization of a bicyclo[3.3.0]octene intermediate obtained from cyclooctadiene to pursue an asymmetric synthesis. The synthesized metabolites were applied in targeted lipidomics to prove lipid peroxidation in edible oils of commercial nutraceuticals.
A Novel Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA1), UCM-05194, Shows Efficacy in Neuropathic Pain Amelioration
González-Gil, Inés,Zian, Debora,Vázquez-Villa, Henar,Hernández-Torres, Gloria,Martínez, R. Fernando,Khiar-Fernández, Nora,Rivera, Richard,Kihara, Yasuyuki,Devesa, Isabel,Mathivanan, Sakthikumar,Del Valle, Cristina Rosell,Zambrana-Infantes, Emma,Puigdomenech, María,Cincilla, Giovanni,Sanchez-Martinez, Melchor,Rodríguez De Fonseca, Fernando,Ferrer-Montiel, Antonio V.,Chun, Jerold,López-Vales, Rubén,López-Rodríguez, María L.,Ortega-Gutiérrez, Silvia
supporting information, p. 2372 - 2390 (2020/01/02)
Neuropathic pain (NP) is a complex chronic pain state with a prevalence of almost 10% in the general population. Pharmacological options for NP are limited and weakly effective, so there is a need to develop more efficacious NP attenuating drugs. Activation of the type 1 lysophosphatidic acid (LPA1) receptor is a crucial factor in the initiation of NP. Hence, it is conceivable that a functional antagonism strategy could lead to NP mitigation. Here we describe a new series of LPA1 agonists among which derivative (S)-17 (UCM-05194) stands out as the most potent and selective LPA1 receptor agonist described so far (Emax = 118%, EC50 = 0.24 μM, KD = 19.6 nM; inactive at autotaxin and LPA2-6 receptors). This compound induces characteristic LPA1-mediated cellular effects and prompts the internalization of the receptor leading to its functional inactivation in primary sensory neurons and to an efficacious attenuation of the pain perception in an in vivo model of NP.
CATIONIC LIPID
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Paragraph 0120-0122, (2019/05/10)
The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1a) or a pharmaceutically acceptable salt thereof. (In formula (1a), each of L1 and L2 independently represent an alkylene group having 3-10 carbon atoms; each of R1 and R2 independently represent an alkyl group having 4-22 carbon atoms or an alkenyl group having 4-22 carbon atoms; X1 represents a single bond or -CO-O-; and ring P represents one of formulae (P-1) to (P-5).)(In formulae (P-1) to (P-5), R3 represents an alkyl group having 1-3 carbon atoms.)
Quaternary phosphonium salt modified dendritic polymer preparation and application of
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Paragraph 0146; 0147; 0148, (2018/01/19)
The invention belongs to the technical field of biological materials, and particularly relates to preparation and application of a quaternary phosphonium salt modified dendriform molecule. The invention provides a quaternary phosphonium salt and a prepara
Antidotes to anthrax lethal factor intoxication. Part 2: Structural modifications leading to improved in vivo efficacy
Kim, Seongjin,Jiao, Guan-Sheng,Moayeri, Mahtab,Crown, Devorah,Cregar-Hernandez, Lynne,McKasson, Linda,Margosiak, Stephen A.,Leppla, Stephen H.,Johnson, Alan T.
supporting information; scheme or table, p. 2030 - 2033 (2011/05/02)
New anthrax lethal factor inhibitors (LFIs) were designed based upon previously identified potent inhibitors 1a and 2. Combining the new core structures with modifications to the C2-side chain yielded analogs with improved efficacy in the rat lethal toxin model.
Hydroxamic acid derivatives of 3-Phenyl propionic acids useful as therapeutic agents for treating anthrax poisoning
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Page/Page column 16, (2008/12/07)
Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 3-phenyl-propionic acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the
HYDROXAMIC ACID DERIVATIVES OF ANILINE USEFUL AS THERAPEUTIC AGENTS FOR TREATING ANTHRAX POISONING
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Page/Page column 53-54, (2008/12/07)
Compounds having the formula (I), wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
PYRROLIDIN-2-ONE DERIVATIVES FOR USE AS DP1 RECEPTOR AGONISTS
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Page/Page column 67, (2010/11/08)
The present invention is directed to compounds that may be used as agonists of prostaglandin receptors. More specifically, the specification describes methods and compositions for making and using DP1 receptor agonists that are pyrrolidin-2-one derivatives.
Endothelin antagonist
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, (2008/06/13)
An endothelin antagonist comprising as the active ingredient a prostanoic acid derivative wherein the α-chain has eight or more skeletal carbon atoms.
