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Search results for: AMIDE RECEPTORS
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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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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Effect of treating method on the physicochemical properties of amine-functionalized carbon nanotubes
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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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Moisture damage mechanism and material selection of HMA with amine antistripping agent
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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.
PublicationWe 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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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublicationThe 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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Interactions between amphotericin B 3-(N',N'-dimethylamino)propyl amide and cellular membrane components in Langmuir monolayers
PublicationPublikacja 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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Esters of p-nitrophenol in synthesis of 1-N-monoamide and 1,7-bis-N,N-amide derivatives of 1,4,7,10-tetraazacyclododecane
PublicationW 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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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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Theoretical Study on Interactions of Bicyclic Vasopressin Analogues with Human Neurohypophyseal Hormone 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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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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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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New clicked full agonists of the estrogen receptor β
PublicationA 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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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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Trend research of vitamin D receptor: Bibliometric analysis
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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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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased 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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Pharmacological Classification and Activity Evaluation of Furan and Thiophene Amide Derivatives Applying Semi-Empirical ab initio Molecular Modeling Methods
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Anion binding by p-aminoazobenzene-derived aromatic amides: spectroscopic and electrochemical studies
PublicationThe 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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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
PublicationAmines 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
PublicationThe 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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Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
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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
PublicationIn 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...
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RORα is not a receptor for melatonin (response to DOI 10.1002/bies.201600018)
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Molecular Dynamics of a Vasopressin V2 Receptor in a Phospholipid Bilayer Membrane
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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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The Effect of Long-Term Administration of Fatty Acid Amide Hydrolase Inhibitor URB597 on Oxidative Metabolism in the Heart of Rats with Primary and Secondary Hypertension
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On the relationship between the structural and volumetric properties of solvated metal ions in O-donor solvents using new structural data in amide solvents
PublicationThe structures of the N,N-dimethylformamide (dmf), N,N-dimethylacetamide (dma), and N,N-dimethylpropionamide (dmp) solvated strontium and barium ions have been determined in solution using large angle X-ray scattering and EXAFS spectroscopy. The strontium ion has a mean coordination number (CN) between 6.2 and 6.8, and the barium ion has a mean CN between 7.1 and 7.8 in these amide solvents. The non-integer numbers indicates that...
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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublicationNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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The influence of azide and imidazole on the properties of Mn- and Cd-based networks: conductivity and nonlinear phenomena
PublicationWe report a study on a family of four new Mn- and Cd-azide-imidazolate-based compounds with various crystal architectures. Notably, three of these compounds display noncentrosymmetric crystal arrangements at room temperature, a rare phenomenon in hybrid organic–inorganic materials. Both nonlinear optical (NLO) and electrical phenomena in these compounds are observed. The NLO processes include second and third harmonic generation,...
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Ion-selective electrodes based on p-tert-butyl-homooxacalixarene di(ethyl)amides
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Ion-selective electrodes based on p-tert-butyl-homooxacalixarene di(ethyl) amides
PublicationPochodne dietyloamidowe p-tert-butylodihomooksakaliks[4]arenu (1), p-tert-butyloheksahomotrioksakaliks[3]arenu (2) oraz p-tert-butylokaliks[4]arenu (3) były wykorzystane jako materiał aktywny w membranach elektrod jonoselektywnych w celu sprawdzenia detekcji kationów różnych rodzajów (Na+, K+, Cs+, Mg2+, Ca2+, Mn2+, Cu2+, Zn2+, Cd2+, Pb2+ oraz kation tetrametyloammoniowy). Wyznaczono charakterystyki elektrod oraz współczynniki...
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Amine-functionalized magnetite-silica nanoparticles as effective adsorbent for removal of uranium(VI) ions
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Vitamin D signaling and melanoma: role of vitamin D and its receptors in melanoma progression and management
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Expression and cellular distribution of estrogen and progesterone receptors and the real-time proliferation of porcine cumulus cells
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Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors
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