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Search results for: AMIDE RECEPTORS
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Physical and Thermophysical Properties of 1-Hexyl-1,4-diaza[2.2.2]bicyclooctanium Bis(trifluoromethylsulfonyl)imide Ionic Liquid
PublicationOwing to their unique properties, ionic liquids (ILs) have become a real alternative to organic compounds. Nowadays, ILs are commonly used in a number of areas such as chemical synthesis and separation techniques. However, ionic liquids continue to have a limited applicability in industry because the information on their physical and chemical properties is not readily available. This paper presents, for the first time, the results...
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Singlet Exciton Diffusion in Vacuum-Evaporated Films of Amine-Based Materials as Studied by Photocurrent and Photoluminescence Quenching Methods
PublicationThe singlet exciton diffusion lengths are determined by the photoconductivity as well as the luminescence surface quenching technique, in vacuum‐evaporated layers of (4,4′,4″‐tris(N‐(3‐methylphenyl)‐N‐phenylylamino) triphenylamine) (m‐MTDATA), 4,4′,4″‐tris[2‐naphthyl(phenyl)amino] triphenylamine (2TNATA), and N,N′‐diphenyl‐N,N′‐bis(3‐methylphenyl)‐[1,1′‐biphenyl]‐4,4′‐diamine (TPD) which are frequently used for fabrication of electroluminescent...
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Acid-aided epoxy-amine curing reaction as reflected in epoxy/Fe3O4 nanocomposites: Chemistry, mechanism, and fracture behavior
PublicationThis work seeks to answer the question whether or not the presence of acid functional groups accelerate epoxyamine curing reaction. Epoxy/Fe3O4 nanocomposite was considered as a case, where discussions are based on chemistry, mechanism behind curing reactions and fracture behavior influenced by acid assistance to crosslinking. Fe3O4 magnetic nanoparticles (MNPs) with nanosilica decorative layer (B-MNP) were synthesized and subsequently...
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Direct conversion of secondary phosphine oxides and H-phosphinates with [di(acyloxy)iodo]benzenes to phosphinic and phosphonic amides
PublicationW publikacji przedstawiono metodę pozwalająca na bezpośrednie otrzymywanie amidów kwasu fosfinowego i fosfonowego w reakcji drugorzędowych tlenków fosfin lub H-fosfinianów z [di(acyloksy)iodo]benzenami w obecności amin pierwszo lub drugorzędowych. Wykorzytując silne acylujące właściwości układu [di(acyloksy)iodo]benzen/R2P(O)H.
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DAF - and collagen-binding properties of chimeric Dr fimbriae
PublicationEkspozycja białek heterologicznych na powierzchni mikroorganizmów jest jedną z nowych strategii stosowanych w mikrobiologii, biotechnologii oraz projektowaniu nowoczesnych szczepionek. W niniejszej pracy zbadano możliwość wykorzystania białka podjednostkowego DraE fimbrii Dr uropatogennych szczepów Escherichia coli jako nośnika heterologicznych sekwencji. W rejon odpowiadający N-terminalnej domenie 2 białka DraE wprowadzono epitopową...
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Synthesis and biological activity of novel ester derivatives of N3-(4-metoxyfumaroyl)-(S)-2,3-diaminopropanoic acid containing amide and keto function as inhibitors of glucosamine-6-phosphate synthase
PublicationA short series of novel ester derivatives of N3-4-methoxyfumaroyl-(S)-2,3-diaminopropanoic acid (FMDP) containing amido or keto functions have been designed and synthesized. Their antifungal activity and inhibitory properties toward fungal glucosamine-6-phosphate synthase has also been evaluated. The obtained compounds 11-13 and 15-17 demonstrated good antifunga activity against Candida albicans. Compounds 11-13 displayed also...
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Berry fruit juices protect lymphocytes against DNA damage and ROS formation induced with heterocyclic aromatic amine PhIP
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Thermophysical properties and phase equilibria study of the binary systems {N-hexylquinolinium bis(trifluoromethylsulfonyl)imide+aromatic hydrocarbons, or an alcohol}
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Low-dose radiation accelerates aging of the T-cell receptor repertoire in CBA/Ca mice
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Methylation of estrogen receptor 2 (ESR2) in deep paravertebral muscles and its association with idiopathic scoliosis
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Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties
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Phenylalanine-Based AMPA Receptor Antagonist as the Anticonvulsant Agent with Neuroprotective Activity—In Vitro and In Vivo Studies
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Methodology of Selecting the Optimal Receptor to Create an Electrochemical Immunosensor for Equine Arteritis Virus Protein Detection
PublicationThe study reports a methodology of selecting the optimal receptor to create an electrochemical immunosensor for equine arteritis virus (EAV) protein detection. The detection was based on antigen recognition by antibodies immobilized on gold electrodes. Modification steps were controlled by electrochemical impedance spectroscopy and cyclic voltammetry measurements. In order to obtain the impedance immunosensor with the best parameters,...
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Methodology of Selecting the Optimal Receptor to Create an Electrochemical Immunosensor for Equine Arteritis Virus Protein Detection
PublicationThe study reports a methodology of selecting the optimal receptor to create an electrochemical immunosensor for equine arteritis virus (EAV) protein detection. The detection was based on antigen recognition by antibodies immobilized on gold electrodes. Modification steps were controlled by electrochemical impedance spectroscopy and cyclic voltammetry measurements. In order to obtain the impedance immunosensor with the best parameters,...
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Angiotensin receptor - neprilysin inhibiton (ARNI) – A novel therapeutic concept for management of hypertension and heart failure
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Interactions of fish gelatin and chitosan in uncrosslinked and crosslinked with EDC films: FT-IR study
PublicationFilms based on fish gelatin, chitosan and blend of fish gelatin and chitosan before and after cross-linking with EDC have been characterized by FT-IR spectroscopy. The FT-IR spectrum of fish gelatin film showed the characteristic amide I, amide II and amide III bands, and the FT-IR spectrum of chitosan film confirmed that the polymer was only a partially deacetylated product, and included CH3-C=O and NH2 groups, the latter both...
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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublicationBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Ionogel fibres of bis(trifluoromethanesulfonyl)imide anion-based ionic liquids for the headspace solid-phase microextraction of chlorinated organic pollutants
PublicationIonogels, a family of hybrid materials in which ionic liquids (ILs) are confined in a sol–gel network, are receiving much attention in a variety of scientific and technological fields. In this work, ionogels derived from three different ILs based on the anion bis(trifluoromethanesulfonyl)imide (TFSI), namely 1-butyl- 3-methylpyridinium bis(trifluoromethanesulfonyl)imide ([C4C1Py][TFSI]), 1-butyl-1-methylpyrrolidinium bis(trifluoromethanesulfonyl)imide...
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Fabrication of high-density nitrogen-vacancy (NV) center-enriched diamond particles through methyl trityl amine (C20H19N) seeding
PublicationDiamond particles (DPs) show promise for advanced applications in bioimaging and quantum sensing due to the presence of defect centers. This work reports a unique growth process for diamond particles composed of nitrogen-vacancy centers (NV-DPs) using a methyl trityl amine (C20H19N) diamondoid seed, which acts as a nitrogen source for NV creation. Growth was performed via microwave plasma-assisted chemical vapor deposition in a...
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Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats
PublicationW pracy przedstawiono wyniki testów otartego pola na zachowanie szczurów po iniekcji zwierzętom WIN55,21-2 (WIN; 3 mg/kg) agonisty receptora kanabinoidowego CB1R, bądź AM4113 (0.3−5.6 mg/kg) przypuszczalnie neutralnego antagonisty receptora kanabinoidowego CB1R oraz mieszaniny obu związków. W badaniach pod uwagę brano następujące zachowania zwierząt; ilość kwadratów, którą szczury przechodziły na czterech nogach, częstotliwość...
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
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Replication study of estrogen receptor 1 XbaI polymorphism in adolescent idiopathic scoliosis (AIS) Caucasian population
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Angiotensin receptor blockers and cancer – Relationship dismissed by VALUE data while waiting for EMA and FDA reports
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Ambulatory Blood Pressure Adds to Explaining Benefits of AT‐1 Receptor Blockade in the Treatment of Left Ventricular Hypertrophy
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Docking is not enough: 17-trifluoromethylphenyl trinor PGF2α is only a very weak ligand of neurokinin-1 receptor
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Correcting a widespread error: Neuroprotectant N-acetyl-L-tryptophan does not bind to the neurokinin-1 receptor
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Phase 3 randomised study of avatrombopag, a novel thrombopoietin receptor agonist for the treatment of chronic immune thrombocytopenia
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Modeling N2O behavior during denitrification with different carbon sources and electron acceptors
PublicationA mathematical model was developed for identification of the most important mechanism leading to nitrous oxide (N2O) accumulation in denitrifying activated sludge systems. The activated sludge model No. 2d (ASM2d) was extended to include intermediate three steps of the denitrification process. The formation and accumulation of nitric oxide (NO) was assumed to be very low in the performed laboratory experiments. These experiments...
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Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats
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Pharmacophore models based studies on the affinity and selectivity toward 5-HT1A with reference to α1-adrenergic receptors among arylpiperazine derivatives of phenytoin
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Can cornelian cherry mask bitter taste of probiotic chocolate? Human TAS2R receptors and a sensory study with comprehensive characterisation of new functional product
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The Leaderless Bacteriocin Enterocin K1 Is Highly Potent against Enterococcus faecium: A Study on Structure, Target Spectrum and Receptor
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Effect of psoriasis activity and topical treatment on plasma epidermal growth factor (EGF) and its soluble receptor (sEGFR)
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XbaI and PvuII Polymorphisms of Estrogen Receptor 1 Gene in Females with Idiopathic Scoliosis: No Association with Occurrence or Clinical Form
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Methylation level of the regulatory regions of the estrogen receptor type 1 gene in paravertebral muscles of girls with idiopathic scoliosis
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Effect of psoriasis activity on epidermal growth factor (EGF) and the concentration of soluble EGF receptor in serum and plaque scales
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Methylation of Estrogen Receptor 1 Gene in the Paraspinal Muscles of Girls with Idiopathic Scoliosis and Its Association with Disease Severity
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
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Vitamin D Receptor Gene Polymorphism and Vitamin D Status in Population of Patients with Cardiovascular Disease—A Preliminary Study
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Nephrotic syndrome unfavorable course correlates with downregulation of podocyte vascular endothelial growth factor receptor (VEGFR)-2
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New generation of analytical tests based on the assessment of enzymatic and nuclear receptor activity changes induced by environmental pollutants
PublicationAnalytical methods show great potential in biological tests. The analysis of biological response that results from environmental pollutant exposure allows: (i) prediction of the risk of toxic effects and (ii) provision of the background for the development of markers of the toxicants presence. Bioanalytical tests based on changes in enzymatic activity and nuclear receptor action provide extremely high specificity and sensitivity....
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Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
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Polymorphism in the chemokine receptor 7 gene (CCR7) is associated with previous myocardial infarction in patients undergoing elective coronary angiography
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Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus
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Molecular dynamics study of 4-OH-phenylacetyl- D -Y(Me)FQNRPR-NH 2 selectivity to V1a receptor
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Does Porcine Oocytes Maturation in Vitro is Regulated by Genes Involved in Transforming Growth Factor Beta Receptor Signaling Pathway?
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Synthesis, activity on NK-3 tachykinin receptor and conformational solution studies of scyliorhinin II analogs modified at position 16
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The acid strength of the HF/AlX3 Lewis-Brønsted complexes involving various electron acceptors as ligands
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(Vapour and liquid) equilibrium in (N,N-dimethylacetamide+methanol+water) at the temperature 313.15 K.
PublicationPraca zawiera wyniki pomiarów całkowitej prężności pary dla tytułowego układu trójskładnikowego oraz dla ''składowych'' układów binarnych. Wyniki obliczeń nadmiarowej energii swobodnej mieszania dla układów (N,N-dimetyloaceta-mid+woda) i (N,N-dimetyloacetamid+metanol) porównane zostały z rezultatami uzyskanymi wcześniej dla innych układów (amid+metanol) oraz (amid+woda). Znaleziono interesującą zależność wartości nadmiaru...
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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublicationFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...