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Wyniki wyszukiwania dla: AMIDE RECEPTORS
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QSPR analysis of some agonists and antagonists of α-adrenergic receptors
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Estrogen receptors genes polymorphisms and age at menarche in idiopathic scoliosis
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Affinity of fentanyl and its derivatives for the σ1-receptor
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Selective detection of F- by chromogenic tetrazole receptor
PublikacjaA chromogenic anion host 4, containing two amide functionalities linked to azo dye and tetrazole rings was synthesized and its complexes with various anions were investigated. The results show that receptor 4 can recognize selectively biologically important F- ion. The binding affinity for F- was investigated by naked-eye colour change, UV-Vis and 1H NMR spectroscopy. Addition F- ion in CH3CN and DMSO to receptor 4 cause a colour...
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Wet H2S corrosion and degradation of pipeline in amine regeneration system
PublikacjaThe paper presents the results of NDT examinations, metallographic tests and risk assessment of degradation related to corrosion of amine regeneration unit in a desulphurisation system. Intensive corrosion resulting from acid gases environment upon water condensation causes perforation of the pipeline. Detailed analysis reveals cracking related to the mechanism of wet H2S. Hydrogen penetration, resulting from the wet H2S process,...
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Hydration of simple amides. FTIR spectra of HDO and theoretical studies
PublikacjaZastosowano metodę ważonych widm różnicowych do opisu hydratacji amidów w roztworach wodnych: formamidu, N-metyloformamidu, N,N-dimetyloformaidu, acetamidu, N-metyloacetamidu, N,N-dimetyloacetamidu. Narzędziem wspomagającym interpretację wyników eksperymentalnych są struktury agregatów solwatacyjnych wokół cząsteczki substancji rozpuszczonej uzyskane na podstawie obliczeń teoretycznych metodą ab initio z korelacją elektronową...
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Atom-economic thiophosphoroselenenylations of C–H acid esters and amides
PublikacjaThree improved thiophosphoroselenenylation procedures of CHacids, including derivatives of malonic and acetyl-, phosphono-, 4-nitrophenyl- and 3-pyridylacetic acids, have been described and compared to previously reported thiophosphoroselenylation of diethyl malonate using bis(disopropoxyphosphinothioyl)diselenide alone or with the aid of methyl iodide. The use of iodine makes it possible to utilize both equivalents of the selenenylating...
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Moving out of CF3‐Land: Synthesis, Receptor Affinity, and in silico Studies of NK1 Receptor Ligands Containing a Pentafluorosulfanyl (SF5) Group
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Neurohypophyseal Receptors-Ligands: Where We Are After the Landmark Rhodopsin Structure Determination
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Molecular Dynamics of Complexes of Atosiban with Neurohypophyseal Receptors in the Fully Hydrated Phospholipid Bilayer
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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Expression of estrogen receptors, PELP1, and SRC in human spermatozoa and their associations with semen quality
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Theoretical Study on Interactions of Bicyclic Vasopressin Analogues with Human Neurohypophyseal Hormone Receptors
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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Moisture damage mechanism and material selection of HMA with amine antistripping agent
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Studies of complexation of metal cations by tris(3,6-dioxaheptyl)amine in solution
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Amine-Based Ionic Liquid for CO2 Capture and Electrochemical or Thermal Regeneration
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Effect of treating method on the physicochemical properties of amine-functionalized carbon nanotubes
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Amine–alkyl derivatives of hydantoin: New tool to combat resistant bacteria
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A convenient method for the preparation of functionalized N-acylsulfenamides from primary amides.
PublikacjaWe have developed a convenient method for the synthesis of functionalized N-acylsulfenamides under mild conditions and in moderate to good yields. The designed method is based on the reaction of (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl)-disulfanyl derivatives with nitrogen nucleophiles generated from primary amides or imides and sodium hydride. The developed method allows for the preparation of N-acylsulfenamides bearing...
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Targeting melanocortin receptor type 1 with small peptides
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Vitamin D receptor(s): In the nucleus but also at membranes?
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Gαi-derived peptide binds the µ-opioid receptor
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Molecular dynamics of fentanyl bound to μ-opioid receptor
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Estrogen Receptor 2 Gene Polymorphism in Idiopathic Scoliosis
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Trend research of vitamin D receptor: Bibliometric analysis
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Towards β-selectivity in functional estrogen receptor antagonists
PublikacjaBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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New clicked full agonists of the estrogen receptor β
PublikacjaA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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N-(2-Arylmethylthio-4-Chloro-5-Methylbenzenesulfonyl)amide Derivatives as Potential Antimicrobial Agents—Synthesis and Biological Studies
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Synthesis and biological evaluation of novel 3,6- amide and thioamide substituted- 2,3,4,9-tetrahydro-1H-carbazoles for anti-cancer activity
PublikacjaHerein, we report the synthesis of new compounds with demonstrated anticancer properties based on the 2,3,4,9- tetrahydro-1H-carbazole scaffold. The Fischer indolization method was used to close the heterocyclic motif. The synthesis method’s scope and limitations were thoroughly assessed through a series of experiments. Biological assays revealed that two thioamide compounds exhibited significant anticancer activity against MCF-7,...
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Esters of p-nitrophenol in synthesis of 1-N-monoamide and 1,7-bis-N,N-amide derivatives of 1,4,7,10-tetraazacyclododecane
PublikacjaW artykule opisana została synteza acylowych pochodnych 1,4,7,10-tetraazacyklododekanu przy pomocy estrów aktywnych. W bezpośredniej reakcji estrów 4-nitrofenylowych z cyklenem prowadzonej w bardzo łagodnych warunkach otrzymano pochodne mono i dipodstawienia z bardzo dobrymi wydajnościami. Zbadano również wpływ różnych parametrów na dystrybucję produktów.
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Interactions between amphotericin B 3-(N',N'-dimethylamino)propyl amide and cellular membrane components in Langmuir monolayers
PublikacjaPublikacja zawiera charakterystykę monowarstw Langmuir'a tworzonych przez pochodną amfoterycyny B tj.amid 3-(N',N'-dimetyloamino)propylowy (AMA) oraz wyniki badań nad jej oddziaływaniem z cholesterolem, ergosterolem i fosfolipidami. Znaleziono, iż stan jonowy cząsteczki pochodnej AMA, a także jej wielkość mają znaczący wpływ na właściwości biologiczne związku.
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Pharmacological Classification and Activity Evaluation of Furan and Thiophene Amide Derivatives Applying Semi-Empirical ab initio Molecular Modeling Methods
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Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
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Amine-Catalyzed Direct Aldol Reactions of Hydroxy- and Dihydroxyacetone: Biomimetic Synthesis of Carbohydrates
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Chemical Derivatization Processes Applied to Amine Determination in Samples of Different Matrix Composition
PublikacjaAmines are important biological compounds, and so their analysis and monitoring in various matrices is worthy of investigation and development.Due to the polar nature of amines, chromatographic analysis of free amines is generally unsatisfactory owing to adsorption and decomposition of the solute on the column, resulting in peak tailing and losses. Therefore, many derivatization reactions are employed to reduce the polarity, improve...
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The impact of cold plasma on the phenolic composition and biogenic amine content of red wine
PublikacjaThe effect of cold plasma (CP) on phenolic compound (PC) and biogenic amine (BA) contents of red wine was investigated for the first time. The influence of CP was compared with the effects of a wine preservation using potassium metabisulfite and a combined method. The PC profile was determined by UPLC-PDA-MS/MS while BAs using DLLME-GC–MS. Chemometric analysis also was used. The content of PCs was 3.1% higher in the sample preserved...
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Anion binding by p-aminoazobenzene-derived aromatic amides: spectroscopic and electrochemical studies
PublikacjaThe synthesis and complexing properties of p-aminoazobenzene-derived mono-, bis-, and trisamides were described. Ligands 3 and 4 bind anions, including fluorides, chlorides, bromides, acetates, benzoates, dihydrogen phosphates, hydrogen sulfates, and p-toluenesulfonates, in chloroform forming 1 : 1 complexes. The highest value of stability constant was evaluated for the 4-F− complex (log K = 5.63 ± 0.21). On the basis of 1H NMR,...
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RORα is not a receptor for melatonin (response to DOI 10.1002/bies.201600018)
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Tuning the sumanene receptor structure towards the development of potentiometric sensors
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Vitamin D receptor gene polymorphisms in Alzheimer's disease patients
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
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Molecular Dynamics of a Vasopressin V2 Receptor in a Phospholipid Bilayer Membrane
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Thermodynamic study of binary mixtures of 2-propanol with ionic liquids, 1-hexyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide, 1-hexyl-3-methylimidazolium trifluoromethanesulfonate and triethylhexylammonium bis(trifluoromethylsulfonyl)imide
PublikacjaIn this work, densities, speeds of sound, refractive indices and viscosities of three binary mixtures containing the ionic liquids 1-hexyl-3-methylimidazolium bis(trifluoromethyl-sulfonyl)imide, 1-hexyl-3-methylimidazolium trifluoromethanesulfonate and triethylhexyl-ammonium bis(trifluoromethylsulfonyl)imide, mixed with 2-propanol at wide temperature and composition ranges at atmospheric pressure have been measured. From these...