Imidazoles
Clotrimazole
Heme
Ketoconazole
Hydrogen-Ion Concentration
Nylons
Binding Sites
Molecular Structure
Magnetic Resonance Spectroscopy
Models, Molecular
Hemeproteins
Catalysis
Crystallography, X-Ray
Antifungal Agents
RNA, Transfer, Asp
Tetragastrin
Copper
Myoglobin
Hydrogen Bonding
Whales
Large marine mammals of the order CETACEA. In the past, they were commercially valued for whale oil, for their flesh as human food and in ANIMAL FEED and FERTILIZERS, and for baleen. Today, there is a moratorium on most commercial whaling, as all species are either listed as endangered or threatened.
Electron Spin Resonance Spectroscopy
A technique applicable to the wide variety of substances which exhibit paramagnetism because of the magnetic moments of unpaired electrons. The spectra are useful for detection and identification, for determination of electron structure, for study of interactions between molecules, and for measurement of nuclear spins and moments. (From McGraw-Hill Encyclopedia of Science and Technology, 7th edition) Electron nuclear double resonance (ENDOR) spectroscopy is a variant of the technique which can give enhanced resolution. Electron spin resonance analysis can now be used in vivo, including imaging applications such as MAGNETIC RESONANCE IMAGING.
Metalloporphyrins
Protein Conformation
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
Protons
Ligands
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Chemistry
Spectrum Analysis, Raman
Spectrum Analysis
Chemical Phenomena
Oleanolic Acid
Spectrophotometry
Thermotoga maritima
A rod-shaped bacterium surrounded by a sheath-like structure which protrudes balloon-like beyond the ends of the cell. It is thermophilic, with growth occurring at temperatures as high as 90 degrees C. It is isolated from geothermally heated marine sediments or hot springs. (From Bergey's Manual of Determinative Bacteriology, 9th ed)
Structure-Activity Relationship
Stereoisomerism
Models, Chemical
Alkylation
X-Ray Absorption Spectroscopy
Prostanoic Acids
Protein Binding
Oxidation-Reduction
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
Horses
Guaiacol
Spectroscopy, Mossbauer
A spectroscopic technique which uses the Mossbauer effect (inelastic scattering of gamma radiation resulting from interaction with heavy nuclei) to monitor the small variations in the interaction between an atomic nucleus and its environment. Such variations may be induced by changes in temperature, pressure, chemical state, molecular conformation, molecular interaction, or physical site. It is particularly useful for studies of structure-activity relationship in metalloproteins, mobility of heavy metals, and the state of whole tissue and cell membranes.
Cytochrome P-450 Enzyme System
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
Receptors, Histamine H3
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Cyanides
Thromboxanes
Physiologically active compounds found in many organs of the body. They are formed in vivo from the prostaglandin endoperoxides and cause platelet aggregation, contraction of arteries, and other biological effects. Thromboxanes are important mediators of the actions of polyunsaturated fatty acids transformed by cyclooxygenase.
Azurin
A bacterial protein from Pseudomonas, Bordetella, or Alcaligenes which operates as an electron transfer unit associated with the cytochrome chain. The protein has a molecular weight of approximately 16,000, contains a single copper atom, is intensively blue, and has a fluorescence emission band centered at 308nm.
Leghemoglobin
Carbon Monoxide
Carbon monoxide (CO). A poisonous colorless, odorless, tasteless gas. It combines with hemoglobin to form carboxyhemoglobin, which has no oxygen carrying capacity. The resultant oxygen deprivation causes headache, dizziness, decreased pulse and respiratory rates, unconsciousness, and death. (From Merck Index, 11th ed)
Cyclization
Enzyme Inhibitors
Zinc
A metallic element of atomic number 30 and atomic weight 65.38. It is a necessary trace element in the diet, forming an essential part of many enzymes, and playing an important role in protein synthesis and in cell division. Zinc deficiency is associated with ANEMIA, short stature, HYPOGONADISM, impaired WOUND HEALING, and geophagia. It is known by the symbol Zn.
Nickel
DNA-Formamidopyrimidine Glycosylase
Indicators and Reagents
Substances used for the detection, identification, analysis, etc. of chemical, biological, or pathologic processes or conditions. Indicators are substances that change in physical appearance, e.g., color, at or approaching the endpoint of a chemical titration, e.g., on the passage between acidity and alkalinity. Reagents are substances used for the detection or determination of another substance by chemical or microscopical means, especially analysis. Types of reagents are precipitants, solvents, oxidizers, reducers, fluxes, and colorimetric reagents. (From Grant & Hackh's Chemical Dictionary, 5th ed, p301, p499)
Pyridines
Amines
Buffers
Spectrophotometry, Ultraviolet
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Tinea
Thermodynamics
A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)
Temperature
Heterocyclic Compounds
Alkanesulfonates
Substrate Specificity
Metmyoglobin
Histamine
Coordination Complexes
Neutral or negatively charged ligands bonded to metal cations or neutral atoms. The number of ligand atoms to which the metal center is directly bonded is the metal cation's coordination number, and this number is always greater than the regular valence or oxidation number of the metal. A coordination complex can be negative, neutral, or positively charged.
Amino Acid Sequence
Diethyl Pyrocarbonate
Explosive Agents
Substances that are energetically unstable and can produce a sudden expansion of the material, called an explosion, which is accompanied by heat, pressure and noise. Other things which have been described as explosive that are not included here are explosive action of laser heating, human performance, sudden epidemiological outbreaks, or fast cell growth.
Nuclear Magnetic Resonance, Biomolecular
Iron
Cobalt
Porphyrins
A group of compounds containing the porphin structure, four pyrrole rings connected by methine bridges in a cyclic configuration to which a variety of side chains are attached. The nature of the side chain is indicated by a prefix, as uroporphyrin, hematoporphyrin, etc. The porphyrins, in combination with iron, form the heme component in biologically significant compounds such as hemoglobin and myoglobin.
Histamine Antagonists
FIGLU Test
Organometallic Compounds
Tubercidin
Tolazoline
A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn.
Mutagenesis, Site-Directed
Ribonuclease, Pancreatic
Dihydropteridine Reductase
Catalytic Domain
Chromatography, High Pressure Liquid
Nitrilotriacetic Acid
Purines
Ergosterol
Camphor 5-Monooxygenase
A soluble cytochrome P-450 enzyme that catalyzes camphor monooxygenation in the presence of putidaredoxin, putidaredoxin reductase, and molecular oxygen. This enzyme, encoded by the CAMC gene also known as CYP101, has been crystallized from bacteria and the structure is well defined. Under anaerobic conditions, this enzyme reduces the polyhalogenated compounds bound at the camphor-binding site.
Bromine
Alkanesulfonic Acids
Crystallization
Rabbits
Escherichia coli
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Medetomidine
Thromboxane-A Synthase
Electrons
Stable elementary particles having the smallest known negative charge, present in all elements; also called negatrons. Positively charged electrons are called positrons. The numbers, energies and arrangement of electrons around atomic nuclei determine the chemical identities of elements. Beams of electrons are called CATHODE RAYS.
Amino Acids
Metals
Cattle
Cytochrome c Group
Candidiasis, Cutaneous
Candida albicans
Ribonucleotides
Circular Dichroism
Acetone
Nitric Oxide Synthase
Electrochemistry
Microsomes, Liver
Isomerism
p38 Mitogen-Activated Protein Kinases
A mitogen-activated protein kinase subfamily that regulates a variety of cellular processes including CELL GROWTH PROCESSES; CELL DIFFERENTIATION; APOPTOSIS; and cellular responses to INFLAMMATION. The P38 MAP kinases are regulated by CYTOKINE RECEPTORS and can be activated in response to bacterial pathogens.
Chemistry, Physical
Aflatoxin B1
A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Oxygen
Quantum Theory
Cytochromes c2
Carbonic Anhydrases
N-Glycosyl Hydrolases
Papain
Deuterium Exchange Measurement
Theophylline
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
Fungicides, Industrial
Propylene Glycol
X-Ray Diffraction
The scattering of x-rays by matter, especially crystals, with accompanying variation in intensity due to interference effects. Analysis of the crystal structure of materials is performed by passing x-rays through them and registering the diffraction image of the rays (CRYSTALLOGRAPHY, X-RAY). (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Physicochemical Phenomena
Cations, Divalent
Thromboxane A2
Receptors, Histamine
Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.
Nicotinic Acids
Ions
Hydrogen
The first chemical element in the periodic table. It has the atomic symbol H, atomic number 1, and atomic weight [1.00784; 1.00811]. It exists, under normal conditions, as a colorless, odorless, tasteless, diatomic gas. Hydrogen ions are PROTONS. Besides the common H1 isotope, hydrogen exists as the stable isotope DEUTERIUM and the unstable, radioactive isotope TRITIUM.
Water
Spectrophotometry, Infrared
Carboxylic Acids
beta-Glucosidase
Ruthenium
Base Sequence
Regulation and function of family 1 and family 2 UDP-glucuronosyltransferase genes (UGT1A, UGT2B) in human oesophagus. (1/8081)
Human UDP-glucuronosyltransferases (UGTs) are expressed in a tissue-specific fashion in hepatic and extrahepatic tissues [Strassburg, Manns and Tukey (1998) J. Biol. Chem. 273, 8719-8726]. Previous work suggests that these enzymes play a protective role in chemical carcinogenesis [Strassburg, Manns and Tukey (1997) Cancer Res. 57, 2979-2985]. In this study, UGT1 and UGT2 gene expression was investigated in human oesophageal epithelium and squamous-cell carcinoma in addition to the characterization of individual UGT isoforms using recombinant protein. UGT mRNA expression was characterized by duplex reverse transcriptase-PCR analysis and revealed the expression of UGT1A7, UGT1A8, UGT1A9 and UGT1A10 mRNAs. UGT1A1, UGT1A3, UGT1A4, UGT1A5 and UGT1A6 transcripts were not detected. UGT2 expression included UGT2B7, UGT2B10 and UGT2B15, but UGT2B4 mRNA was absent. UGT2 mRNA was present at significantly lower levels than UGT1 transcripts. This observation was in agreement with the analysis of catalytic activities in oesophageal microsomal protein, which was characterized by high glucuronidation rates for phenolic xenobiotics, all of which are classical UGT1 substrates. Whereas UGT1A9 was not regulated, differential regulation of UGT1A7 and UGT1A10 mRNA was observed between normal oesophageal epithelium and squamous-cell carcinoma. Expression and analysis in vitro of recombinant UGT1A7, UGT1A9, UGT1A10, UGT2B7 and UGT2B15 demonstrated that UGT1A7, UGT1A9 and UGT1A10 catalysed the glucuronidation of 7-hydroxybenzo(alpha)pyrene, as well as other environmental carcinogens, such as 2-hydroxyamino-1-methyl-6-phenylimidazo-(4, 5-beta)-pyridine. Although UGT1A9 was not regulated in the carcinoma tissue, the five-fold reduction in 7-hydroxybenzo(alpha)pyrene glucuronidation could be attributed to regulation of UGT1A7 and UGT1A10. These data elucidate an individual regulation of human UGT1A and UGT2B genes in human oesophagus and provide evidence for specific catalytic activities of individual human UGT isoforms towards environmental carcinogens that have been implicated in cellular carcinogenesis. (+info)Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor, SB203580. (2/8081)
SB203580 (4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imi dazole) is widely used as a specific inhibitor of p38 mitogen-activated protein kinase (MAPK). Here, we report that SB203580 activates the serine/threonine kinase Raf-1 in quiescent smooth muscle cells in a dose-dependent fashion. The concentrations of SB203580 required lie above those necessary to inhibit p38 MAPK and we were unable to detect basal levels of active p38 MAPK. SB203580 does not directly activate Raf-1 in vitro, and fails to activate Ras, MEK, and ERK in intact cells. In vitro, however, SB203580-stimulated Raf-1 activates MEK1 in a coupled assay. We conclude that activation of Raf-1 by SB203580 is not mediated by an inhibition of p38 MAPK, is Ras-independent, and is uncoupled from MEK/ERK signaling. (+info)An inhibitor of p38 mitogen-activated protein kinase protects neonatal cardiac myocytes from ischemia. (3/8081)
Cellular ischemia results in activation of a number of kinases, including p38 mitogen-activated protein kinase (MAPK); however, it is not yet clear whether p38 MAPK activation plays a role in cellular damage or is part of a protective response against ischemia. We have developed a model to study ischemia in cultured neonatal rat cardiac myocytes. In this model, two distinct phases of p38 MAPK activation were observed during ischemia. The first phase began within 10 min and lasted less than 1 h, and the second began after 2 h and lasted throughout the ischemic period. Similar to previous studies using in vivo models, the nonspecific activator of p38 MAPK and c-Jun NH2-terminal kinase, anisomycin, protected cardiac myocytes from ischemic injury, decreasing the release of cytosolic lactate dehydrogenase by approximately 25%. We demonstrated, however, that a selective inhibitor of p38 MAPK, SB 203580, also protected cardiac myocytes against extended ischemia in a dose-dependent manner. The protective effect was seen even when the inhibitor was present during only the second, sustained phase of p38 MAPK activation. We found that ischemia induced apoptosis in neonatal rat cardiac myocytes and that SB 203580 reduced activation of caspase-3, a key event in apoptosis. These results suggest that p38 MAPK induces apoptosis during ischemia in cardiac myocytes and that selective inhibition of p38 MAPK could be developed as a potential therapy for ischemic heart disease. (+info)In vivo demonstration of H3-histaminergic inhibition of cardiac sympathetic stimulation by R-alpha-methyl-histamine and its prodrug BP 2.94 in the dog. (4/8081)
1. The aim of this study was to investigate whether histamine H3-receptor agonists could inhibit the effects of cardiac sympathetic nerve stimulation in the dog. 2. Catecholamine release by the heart and the associated variation of haemodynamic parameters were measured after electrical stimulation of the right cardiac sympathetic nerves (1-4 Hz, 10 V, 10 ms) in the anaesthetized dog treated with R-alpha-methyl-histamine (R-HA) and its prodrug BP 2.94 (BP). 3. Cardiac sympathetic stimulation induced a noradrenaline release into the coronary sinus along with a tachycardia and an increase in left ventricular pressure and contractility without changes in mean arterial pressure. Intravenous administration of H3-receptor agonists significantly decreased noradrenaline release by the heart (R-HA at 2 micromol kg(-1) h(-1): +77 +/- 25 vs +405 +/- 82; BP 2.94 at 1 mg kg(-1): +12 +/- 11 vs +330 +/- 100 pg ml(-1) in control conditions, P < or = 0.05), and increases in heart rate (R-HA at 2 micromol kg(-1) h(-1): +26 +/- 8 vs +65 +/- 10 and BP 2.94 at 1 mg kg(-1): +30 +/- 8 vs 75 +/- 6 beats min(-1), in control conditions P < or = 0.05), left ventricular pressure, and contractility. Treatment with SC 359 (1 mg kg(-1)) a selective H3-antagonist, reversed the effects of H3-receptor agonists. Treatment with R-HA at 2 micromol kg(-1) h(-1) and BP 2.94 at 1 mg kg(-1) tended to decrease, while that with SC 359 significantly increased basal heart rate (from 111 +/- 3 to 130 +/- 5 beats min(-1), P < or = 0.001). 4. Functional H3-receptors are present on sympathetic nerve endings in the dog heart. Their stimulation by R-alpha-methyl-histamine or BP 2.94 can inhibit noradrenaline release by the heart and its associated haemodynamic effects. (+info)p38 but not p44/42 mitogen-activated protein kinase is required for nitric oxide synthase induction mediated by lipopolysaccharide in RAW 264.7 macrophages. (5/8081)
Protein kinase C (PKC)-alpha, -betaI, and -delta are known to be involved in the lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages. The role of mitogen-activated protein kinases (MAPK) p44/42 and p38 in the LPS effect was studied further. LPS-mediated NO release and the inducible form of NO synthase expression were inhibited by the p38 inhibitor, SB 203580, but not by the MAPK kinase inhibitor, PD 98059. Ten-minute treatment of cells with LPS resulted in the activation of p44/42 MAPK, p38, and c-Jun NH2-terminal kinase. Marked or slight activation, respectively, of p44/42 MAPK or p38 was also seen after 10-min treatment with 12-O-tetradecanoylphorbol-13-acetate, but c-Jun NH2-terminal kinase activation did not occur. Tyrosine kinase inhibitor, genestein, attenuated the LPS-induced activation of both p44/42 MAPK and p38, whereas the PKC inhibitors, Ro 31-8220 and calphostin C, or long-term treatment with 12-O-tetradecanoylphorbol-13-acetate resulted in inhibition of p44/42 MAPK activation, but had only a slight effect on p38 activation, indicating that LPS-mediated PKC activation resulted in the activation of p44/42 MAPK. Nuclear factor-kappaB (NF-kappaB)-specific DNA-protein-binding activity in the nuclear extracts was enhanced by 10-min, 1-h, or 24-h treatment with LPS. Analysis of the proteins involved in NF-kappaB binding showed translocation of p65 from the cytosol to the nucleus after 10-min treatment with LPS. The onset of NF-kappaB activation correlated with the cytosolic degradation of both inhibitory proteins of NF-kappaB, IkappaB-alpha and IkappaB-beta. IkappaB-alpha was resynthesized rapidly after loss (1-h LPS treatment), whereas IkappaB-beta levels were not restored until after 24-h treatment. SB 203580 but not PD 98059 inhibited the LPS-induced stimulation of NF-kappaB DNA-protein binding. Thus, activation of p38 but not p44/42 MAPK by LPS resulted in the stimulation of NF-kappaB-specific DNA-protein binding and the subsequent expression of inducible form of NO synthase and NO release in RAW 264.7 macrophages. (+info)Conformation-dependent inhibition of gastric H+,K+-ATPase by SCH 28080 demonstrated by mutagenesis of glutamic acid 820. (6/8081)
Gastric H+,K+-ATPase can be inhibited by imidazo pyridines like 2-methyl-8-[phenylmethoxy] imidazo-(1,2a) pyridine 3-acetonitrile (SCH 28080). The drug shows a high affinity for inhibition of K+-activated ATPase and for prevention of ATP phosphorylation. The inhibition by SCH 28080 can be explained by assuming that SCH 28080 binds to both the E2 and the phosphorylated intermediate (E2-P) forms of the enzyme. We observed recently that some mutants, in which glutamic acid 820 present in transmembrane domain six of the catalytic subunit had been replaced (E820Q, E820N, E820A), lost their K+-sensitivity and showed constitutive ATPase activity. This ATPase activity could be inhibited by similar SCH 28080 concentrations as the K+-activated ATPase of the wild-type enzyme. SCH 28080 also inhibited ATP phosphorylation at 21 degrees C of the mutants E820D, E820N, and E820A, although with varying efficacy and affinity. ATP-phosphorylation of mutant E820Q was not inhibited by SCH 28080; in contrast, the phosphorylation level at 21 degrees C was nearly doubled. These findings can be explained by assuming that mutation of Glu820 favors the E1 conformation in the order E820Q >E820A >E820N >wild-type = E820D. The increase in the phosphorylation level of the E820Q mutant can be explained by assuming that during the catalytic cycle the E2-P intermediate forms a complex with SCH 28080. This intermediate hydrolyzes considerably slower than E2-P and thus accumulates. The high tendency of the E820Q mutant for the E1 form is further supported by experiments showing that ATP phosphorylation of this mutant is rather insensitive towards vanadate, inorganic phosphate, and K+. (+info)Signal transduction triggered by lipid A-like molecules in 70Z/3 pre-B lymphocyte tumor cells. (7/8081)
The lipid A (endotoxin) moiety of lipopolysaccharide (LPS) elicits rapid cellular responses from many cell types, including macrophages, lymphocytes, and monocytes. In CD14 transfected 70Z/3 pre-B lymphocyte tumor cells, these responses include activation of the MAP kinase homolog, p38, activation of NF-kappaB, and transcription of kappa light chains, leading to the assembly of surface IgM. In this work, we explored the specificity of the response with regard to lipid structure, and the requirement for p38 kinase activity prior to NF-kappaB activation in control and CD14 transfected 70Z/3 (CD14-70Z/3) cells. A p38-specific inhibitor, SB203580, was used to block p38 kinase activity in cells. CD14-70Z/3 cells were incubated with 1-50 microM SB203580, and then stimulated with LPS. Nuclear extracts were prepared, and NF-kappaB activation was measured using an electrophoretic mobility shift assay. SB203580 did not inhibit LPS induced NF-kappaB activation. In addition, LPS failed to activate p38 tyrosine phosphorylation in 70Z/3 cells lacking CD14, in spite of rapid NF-kappaB activation and robust surface IgM production with appropriate higher doses of LPS. LPS stimulation of p38 phosphorylation, NF-kappaB activation, and surface IgM expression were all blocked completely by lipid A-like endotoxin antagonists whether or not CD14 was present. Acidic glycerophospholipids and ceramides did not mimic lipid A-like molecules either as agonists or antagonists in this system. Our data support the hypothesis that lipid A-mediated activation of cells requires stimulation of a putative lipid A sensor that is downstream of CD14, but upstream of p38 and NF-kappaB. (+info)A chimeric gastric H+,K+-ATPase inhibitable with both ouabain and SCH 28080. (8/8081)
2-Methyl-8-(phenylmethoxy)imidazo(1,2-a)pyridine-3acetonitrile+ ++ (SCH 28080) is a K+ site inhibitor specific for gastric H+,K+-ATPase and seems to be a counterpart of ouabain for Na+,K+-ATPase from the viewpoint of reaction pattern (i.e. reversible binding, K+ antagonism, and binding on the extracellular side). In this study, we constructed several chimeric molecules between H+,K+-ATPase and Na+,K+-ATPase alpha-subunits by using rabbit H+,K+-ATPase as a parental molecule. We found that the entire extracellular loop 1 segment between the first and second transmembrane segments (M1 and M2) and the luminal half of the M1 transmembrane segment of H+, K+-ATPase alpha-subunit were exchangeable with those of Na+, K+-ATPase, respectively, preserving H+,K+-ATPase activity, and that these segments are not essential for SCH 28080 binding. We found that several amino acid residues, including Glu-822, Thr-825, and Pro-829 in the M6 segment of H+,K+-ATPase alpha-subunit are involved in determining the affinity for this inhibitor. Furthermore, we found that a chimeric H+,K+-ATPase acquired ouabain sensitivity and maintained SCH 28080 sensitivity when the loop 1 segment and Cys-815 in the loop 3 segment of the H+,K+-ATPase alpha-subunit were simultaneously replaced by the corresponding segment and amino acid residue (Thr) of Na+,K+-ATPase, respectively, indicating that the binding sites of ouabain and SCH 28080 are separate. In this H+, K+-ATPase chimera, 12 amino acid residues in M1, M4, and loop 1-4 that have been suggested to be involved in ouabain binding of Na+, K+-ATPase alpha-subunit are present; however, the low ouabain sensitivity indicates the possibility that the sensitivity may be increased by additional amino acid substitutions, which shift the overall structural integrity of this chimeric H+,K+-ATPase toward that of Na+,K+-ATPase. (+info)51605-32-4,1H-Imidazole-5-carboxylicacid, 4-methyl-, ethyl ester
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Imidazole
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WHOCC - ATC/DDD Index
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Patent US4532331 - 1-Benzyl-2-aminomethyl imidazole derivatives - Google Patents
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Physical Properties and CO2 Reaction Pathway of 1-Ethyl-3-Methylimidazolium Ionic Liquids with Aprotic Heterocyclic Anions ...
Separation of imidazole and its derivatives by capillary electrophoresis | [email protected]
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IUCr) 2-[2-(5-Bromo-thio-phen-2-yl)-4,5-di-phenyl-1H-imidazol-1-yl]-3-phenyl-propan-1-ol
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Imidazolone
doi:10.1007/s10593-015-1716-3. (Imidazoles). ...
Ketoconazole
It is an imidazole and works by hindering the production of ergosterol required for the fungal cell membrane, thereby slowing ... As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a ... Ketoconazole is a synthetic imidazole. It is a nonsteroidal compound. It is a racemic mixture of two enantiomers, ... 586-. ISBN 978-3-88763-075-1. Heeres J, Backx LJ, Mostmans JH, Van Cutsem J (August 1979). "Antimycotic imidazoles. part 4. ...
Medication
Anti-fungal: imidazoles, polyenes. Anti-inflammatory: NSAIDs, corticosteroids. Anti-allergy: mast cell inhibitors. Anti- ...
Glyoxal
... is a valuable building block in organic synthesis, especially in the synthesis of heterocycles such as imidazoles. A ... Snyder, H. R.; Handrick, R. G.; Brooks, L. A. (1942). "Imidazole". Organic Syntheses. 22: 65.; Collective Volume, vol. 3, p. ...
Nitrate ester
Snyder, H. R.; Handrick, R. G.; Brooks, L. A. (1942). "Imidazole". Organic Syntheses.; Collective Volume, vol. 3, p. 471 Alvin ...
Cadmium tetrafluoroborate
J., Reedijk; G.C., Verschoor (1973-04-15). "Pyrazoles and imidazoles as ligands. XX. The crystal and molecular structure of ... octahedral geometries for Cadmium tetrafluoroborate complexes with nitrogen-containing ligands such as pyrazoles and imidazoles ...
5-Fluorowillardiine
Purines, pyrimidines, and imidazoles. Part XVII. A synthesis of willardiine". Journal of the Chemical Society (Resumed): 583. ...
1-Methylimidazole
With the N-methyl group, this particular derivative of imidazole cannot tautomerize. It is slightly more basic than imidazole, ... Reedijk,R. (1969). "Pyrazoles and imidazoles as ligands. II. Coordination compounds of N-methyl imidazole with metal ... The main one is acid-catalysed methylation of imidazole by methanol. The second method involves the Radziszewski reaction from ... Similarly, 1-methylimidazole may be synthesized by first deprotonating imidazole to form a sodium salt followed by methylation ...
Dazoxiben
1. Imidazole derivatives". Journal of Medicinal Chemistry. 24 (10): 1139. doi:10.1021/jm00142a005. PMID 7199088. Cross, Peter E ... One convenient synthesis starts with the O-chloroethyl ether of p-hydroxybenzamide and proceeds bydisplacement with imidazole ... 1. 1-[(Aryloxy)alkyl]-1H-imidazoles". Journal of Medicinal Chemistry. 28 (10): 1427. doi:10.1021/jm00148a009. PMID 3930740. v t ... Imidazoles, Benzoic acids, All stub articles, Blood and blood forming organ drug stubs). ...
Tinidazole
Ebel K, Koehler H, Gamer AO, Jäckh R (2002). "Imidazole and Derivatives.". In Ullmann's Encyclopedia of Industrial Chemistry. ...
Tioconazole
... is an antifungal medication of the imidazole class used to treat infections caused by a fungus or yeast. It is ... Antimycotic imidazole derivative. A displacement reaction between 1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethanol and 2- ... Imidazole antifungals, Lanosterol 14α-demethylase inhibitors, Thiophenes). ...
Benzimidazole
This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a colorless solid. ... doi:10.1002/14356007.a16_487.pub2 Grimmett, M. R. (1997). Imidazole and benzimidazole synthesis. Boston: Academic Press. ISBN 0 ...
Benzimidazoline
Grimmett, M. R. (1997). Imidazole and Benzimidazole Synthesis. Academic Press. pp. 71ff. ISBN 9780080534459. (Articles without ...
2-Imidazoline
... (Preferred IUPAC name: 4,5-dihydro-1H-imidazole) is one of three isomers of the nitrogen-containing heterocycle ... Ishihara M, Togo H (2006). "An Efficient Preparation of 2-Imidazolines and Imidazoles from Aldehydes with Molecular Iodine and ... Imidazoles can be prepared from dehydrogenation of imidazolines. As a structural analogue of 2-oxazolines, 2-imidazolines have ...
Dioxins and dioxin-like compounds
These include indoles, flavones, benzoflavones, imidazoles and pyridines. These compounds are metabolized rapidly, but ...
Flutrimazole
... is an imidazole derivative. Its antifungal activity has been demonstrated in in vivo and in vitro studies to be ... Imidazole antifungals, Lanosterol 14α-demethylase inhibitors, All stub articles, Antiinfective agent stubs, Genito-urinary ...
Acadesine
A novel synthesis of 5-amino-1-(.beta.-D-ribofuranosyl)imidazole-4-carboxamide and 5-amino-1-(.beta.-D-ribopyranosyl)imidazole- ... resulting in the formation of the imidazole ring. Reaction with alkoxide then converts the nitrile nearest the sugar to an ...
Karl Fischer titration
A common base is imidazole. The titration cell also consists of a smaller compartment with a cathode immersed in the anode ...
Genetically modified rice
This variety tolerates imidazole herbicides. It was bred by traditional breeding techniques that are not considered to be ...
Microsporum gypseum
Most of these administered drugs are variants of imidazoles. The treatment of onychomycosis involves the administration of ...
Darshan Ranganathan
She created a protocol which achieved the autonomous reproduction of imidazole, an ingredient of histadine and histamine with ... Ranganathan, Darshan; Rathi, Ramesh (1986). "Imidazole synthesis on a solid support". Tetrahedron Letters. 27 (22): 2491-2492. ...
Mesoionic compounds
... of the imidazole series". The Journal of Organic Chemistry. 36 (22): 3368-3372. doi:10.1021/jo00821a022. ( ...
Oxymetazoline
... is a derivative of imidazole. It was developed from xylometazoline at E. Merck Darmstadt by Wolfgang Fruhstorfer ...
Chichibabin reaction
... imidazole > 3-methylnaphth[1,2-d]imidazole. Since the addition of the amide ion proceeds quickly with these substrates, the ...
Transition metal NHC complex
The imidazole ring of the NHC ligand is angled away from the metal center, yet the substituents at the 1,3 positions of the ... Schaub, Thomas; Radius, Udo (2010). "1,3-Dialkyl-Imidazole-2-Ylidenes". Inorg. Synth. 35: 78-83. doi:10.1002/9780470651568.ch4 ... imidazole ring are angled towards it. The presence of the ligand inside of the metal coordination sphere affects the metal ...
Croconazole
... (INN) is an imidazole antifungal. Pfaller MA (2010). "Chapter 143: Croconazole". In Turner A (ed.). Logan Turner's ... Imidazole antifungals, Lanosterol 14α-demethylase inhibitors, Phenol ethers, All stub articles, Antiinfective agent stubs). ...
Transition metal pyridine complexes
Imidazoles Imidazoles comprise another major series of N-heterocyclic ligands. Unlike pyridines, imidazole derivatives are ... With a pKa of 5.25 for its conjugate acid, pyridine is about 15x less basic than imidazole. Pyridine is a weak pi-acceptor ...
Persistent carbene
Thus, imidazole-2-ylidenes are thermodynamically stable. It had been also conjectured that the double bond between carbons 4 ... A saturation on the carbons 4 and 5 of the imidazole ring, or the lack of a ring structure all together leaves the carbene ... Imidazole-based carbenes are thermodynamically stable and generally have diagnostic 13C NMR chemical shift values between 210 ... Deprotonation with sodium or potassium hydride in a mixture of liquid ammonia/THF at −40 °C has been reported for imidazole- ...
Aromaticity
In imidazole, both nitrogens are sp2-hybridized; the one in the double bond contributes one electron and the one which is not ... Pyrrole and imidazole are both five membered aromatic rings that contain heteroatoms. In pyrrole, each of the four sp2- ... Other examples include pyridine, pyrazine, pyrrole, imidazole, pyrazole, oxazole, thiophene, and their benzannulated analogs ( ...
Allosteric regulation
Rivalta I, Sultan MM, Lee NS, Manley GA, Loria JP, Batista VS (May 2012). "Allosteric pathways in imidazole glycerol phosphate ...
Browsing by Subject "Imidazoles"
Browsing by Subject "Imidazoles"
Tinea Pedis Medication: Topical imidazoles, Topical pyridones, Topical allylamines, Topical benzylamines, Oral antimycotics,...
Topical imidazoles. Class Summary. Topical imidazoles are effective in all forms of tinea pedis but are excellent treatments ... Luliconazole, an imidazole topical cream, is applied once daily for 2 weeks. [18, 19] A patient with chronic hyperkeratotic ( ... Luliconazole is an imidazole antifungal that alters the fungal cell membrane by interacting with 14-alpha demethylase (an ... Ketoconazole is an imidazole broad-spectrum antifungal agent; it inhibits the synthesis of ergosterol, causing cellular ...
1H-Imidazole, 2-ethyl
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
What are the recommendations for pH based elution, as opposed to imidazole? | NEB
RCSB PDB - 4TUV: X-ray crystal structure of CYP119 from Sulfolobus acidocaldarius, complexed with 4-(4-chlorophenyl)imidazole
Arrangements of fluorophores in the salts of imidazole tethered anthracene derivatives with pyridinedicarboxylic acids...
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Condensed Imidazoles, 5-5 Ring Systems - Author: Preston, P. N. - Price: 422,40€ ... Condensed Imidazoles of Type 5-5 with no Additional Heteroatom.. Condensed Imidazoles of Type 5-5 with One Additional ... Condensed Imidazoles of Type 5-5 with Two Additional Heteroatoms.. Condensed Imidazoles of Type 5-5 with Three Additional ... The Chemistry of Heterocyclic Compounds, Condensed Imidazoles, 5-5 Ring Systems. 422,40€ ...
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Identification of a pKa-regulating motif stabilizing imidazole-modified double-stranded DNA
... Dieter Buyst (UGent) , Vicky ... D. Buyst et al., "Identification of a pKa-regulating motif stabilizing imidazole-modified double-stranded DNA," NUCLEIC ACIDS ... Molecular Dynamics, Modified DNA, Imidazole, NMR, MOLECULAR-DYNAMICS SIMULATIONS, PARTICLE MESH EWALD, LOOP-HELIX MOTIF, NMR- ... Tethering histamine to the C5 of the thymine base via an amide bond, allows the flexible positioning of the imidazole function ...
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formation and aerosol growth
Heterogeneous photochemistry of imidazole-2-carboxaldehyde: HO2 radical formation and aerosol growth Laura González Palacios1,2 ... Here we investigate the HO2 radical production from the UV irradiation of imidazole-2-carboxaldehyde (IC) in bulk aqueous films ... Heterogeneous photochemistry of imidazole-2-carboxaldehyde: HO2 radical formation and aerosol growth, Atmos. Chem. Phys., 16, ... including its light-absorbing product imidazole-2-carboxaldehyde (IC). IC is a photosensitizer that can contribute to ...
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Neck dissection and post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin protocol are useful...
... post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin was performed in some patients. The ... et al. Neck dissection and post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin protocol are ... Neck dissection and post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin protocol are useful ... Neck dissection and post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin protocol are useful ...
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A self-cleaving DNA enzyme modified with amines, guanidines and imidazoles operates independently of divalent metal cations (M2...
Herein, dCTP, dATP and dUTP bearing, respectively, a cationic amine, an imidazole and a cationic guanidine, were enzymatically ... A self-cleaving DNA enzyme modified with amines, guanidines and imidazoles operates independently of divalent metal cations ( ... A self-cleaving DNA enzyme modified with amines, guanidines and imidazoles operates independently of divalent metal cations ( ... A self-cleaving DNA enzyme modified with amines, guanidines and imidazoles operates independently of divalent metal cations ( ...
Methyl 1H-imidazole-2-carboxylate - porphyrin-systems
dimethyl 1-(2-oxo-2-phenylethyl)-1H-imidazole-4,5-dicarboxylate AKSci HTS001631
Axinellamines A-D, Novel Imidazo-Azolo-Imidazole Alkaloids from the Australian Marine Skponge Axinells sp.
Four imidazo-azolo-imidazole alkaloids, axinellamines A-D, have been isolated from an Australian marine sponge, Axinella sp. ( ... Three of these compounds had bactericidal activity against Helicobacter pylori at 1000 卮Four imidazo-azolo-imidazole alkaloids ... Axinellamines A-D, Novel Imidazo-Azolo-Imidazole Alkaloids from the Australian Marine Skponge Axinells sp.. ... order: Halichondrida: family: Axinellidae). These compounds contain a unique perhydrocyclopenta-imidazo-azolo-imidazole carbon ...
Efficient incorporation of 1-(2-deoxy-beta-D-ribofuranosyl)-2-oxo-imidazole-4-carboxamide into DNA via a suitable convertible...
2-oxo-imidazole-4-carboxamide (3) is based on the ring contraction of pyrimidine (5-BrdU) into imidazolin-2-one. The ... Abstract : The synthetic scheme of 1-(2-deoxy-beta-D-ribofuranosyl)-2-oxo-imidazole-4-carboxamide (3) is based on the ring ... Efficient incorporation of 1-(2-deoxy-beta-D-ribofuranosyl)-2-oxo-imidazole-4-carboxamide into DNA via a suitable convertible ... Efficient incorporation of 1-(2-deoxy-beta-D-ribofuranosyl)-2-oxo-imidazole-4-carboxamide into DNA via a suitable convertible ...
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View of Profile of the resistance to macrolides and imidazoles of Helicobacter pylori in a sample of the Portuguese population.
One-pot synthesis of β-N-glycosyl imidazole analogues via a palladium-catalysed decarboxylative allylation | NTU Singapore
Xiang, S., He, J., Ma, J., & Liu, X.-W. (2014). One-pot synthesis of β-N-glycosyl imidazole analogues via a palladium-catalysed ... A concise and highly efficient strategy for the synthesis of N-glycosyl imidazole analogues is reported. This reaction is based ... One-pot synthesis of -N-glycosyl imidazole analogues via a palladium-catalysed decarboxylative allylation.pdf. Main article. ... One-pot synthesis of β-N-glycosyl imidazole analogues via a palladium-catalysed decarboxylative allylation. ...
Structural Changes upon Oxygenation of an Iron (II) (porphyrinato) (imidazole) Complex - Fingerprint
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Multifunctional Hydrolytic Catalyses. IV. The Catalytic Hydrolysis of p-Nitrophenyl Acetate by Copolymers Containing...
The acylation rate at the hydroxamate anion unit was affected only insignificantly by the presence of the imidazole unit, and ... The acylation rate at the hydroxamate anion unit was affected only insignificantly by the presence of the imidazole unit, and ... The acylation rate at the hydroxamate anion unit was affected only insignificantly by the presence of the imidazole unit, and ... The acylation rate at the hydroxamate anion unit was affected only insignificantly by the presence of the imidazole unit, and ...
MeSH | Imidazoles (D007093)
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Heterocyclic Compounds1
- These are aromatic heterocyclic compounds containing a purine moiety, which is formed a pyrimidine-ring ring fused to an imidazole ring. (drugbank.com)
Compounds9
- These compounds contain a unique perhydrocyclopenta-imidazo-azolo-imidazole carbon skeleton. (edu.au)
- Three of these compounds had bactericidal activity against Helicobacter pylori at 1000 卮 Four imidazo-azolo-imidazole alkaloids, axinellamines A-D, have been isolated from an Australian marine sponge, Axinella sp. (edu.au)
- compounds containing an imidazole skeleton. (systemsbiology.net)
- As many as three compounds were as active as the standard benznidazole and two others were 2-3-fold more active highlighting the potential of substituted imidazoles, easily accessible from nitroalkenes, as possible anti-parasitic agents. (fiocruz.br)
- For example, the efficacy of the imidazole compounds to restrict Trypanosoma growth in vitro was ≥ 12-fold specific towards T. congolense relative to the mammalian cells. (elsevier.com)
- In particular, three imidazole compounds (C1, C6, and C8) not only cleared the systemic parasite burden but cured infected rats after no death was recorded. (elsevier.com)
- On the other hand, the remaining five imidazole compounds (C2, C3, C4, C5, and C7) drastically reduced the systemic parasite load while extending survival time of the infected rats by 14 days as compared with control. (elsevier.com)
- A second series of compounds was designed as derivatives of a weakly binding ligand containing dansyl, imidazole, and phenol moieties. (niu.edu)
- It contains a 4-carboxylic acid ester-substituted imidazole moiety, which is also present in a number of compounds that are structural variants of the triazolo and imidazolo benzodiazepines. (pharmacy180.com)
Derivatives2
- A series of differently modulated benzo[d]imidazole-2-one derivatives were designed and synthesised. (unito.it)
- Together, findings support the anti-parasitic prospects of the new series of imidazole derivatives. (elsevier.com)
Antifungal2
- Nizral Cream is an imidazole antifungal. (mytestopay.com)
- Naftin Cream is a synthetic allylamine derivative while Ketoconazole is an imidazole antifungal agent. (prescriptionpoint.com)
Derivative1
- In the search for new chemical scaffolds able to afford NLRP3 inflammasome inhibitors, we used a pharmacophore-hybridization strategy by combining the structure of the acrylic acid derivative INF39 with the 1-(piperidin-4-yl)1,3-dihydro-2H-benzo[d]imidazole-2-one substructure present in HS203873, a recently identified NLRP3 binder. (unito.it)
Frameworks2
- Zeolitic imidazole frameworks (ZIF)-8 and polymers are potential platforms for drug delivery purpose. (tdl.org)
- 2020). d-Orbital steered active sites through ligand editing on heterometal imidazole frameworks for rechargeable zinc-air battery . (lightsource.ca)
Hydrogen bond1
- Using NMR and unrestrained molecular dynamics, a structural motif involving the formation of a hydrogen bond between the imidazole and the Hoogsteen side of the guanine bases of two neighboring GC base pairs is established. (ugent.be)
Methyl2
- The 1H-Imidazole,1-methyl-5-nitroso-4-phenyl-, with the CAS registry number 111380-08-6, is also known as 1-Methyl-5-nitroso-4-phenyl-1H-imidazole. (lookchem.com)
- Moreover, (5-(chloromethyl)-2-oxo-1,3-dioxol-4-yl)methyl 1-((2′-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate is also used in the process of Abbreviated New Drug Application (ANDA) filing to FDA and toxicity study of respective drug formulation. (synthinkchemicals.com)
Heterogeneous1
- The synthesis of 2,4,5-triaryl-imidazoles from benzyl, aldehydes and NH 4 OAc, as ammonia source, in the presence of catalytic amount of NiCl 2 ·6H 2 O supported onto acidic alumina in very good yields under heterogeneous system is reported. (edu.au)
Organic1
- The multiphase chemistry of glyoxal is a source of secondary organic aerosol (SOA), including its light-absorbing product imidazole-2-carboxaldehyde (IC). (copernicus.org)
Inhibitors3
- IMSEAR at SEARO: Quantitative structure-activity relationship of 4,5-diphenyl-2-(substituted thio)-1H-imidazoles as the inhibitors of acyl CoA: cholesterol acyltransferase. (who.int)
- Singh P, Kumar R. Quantitative structure-activity relationship of 4,5-diphenyl-2-(substituted thio)-1H-imidazoles as the inhibitors of acyl CoA: cholesterol acyltransferase. (who.int)
- A quantitative structure-activity relationship (QSAR) analysis of 4,5-diphenyl-2-(substituted thio)-1H-imidazoles as the potential inhibitors of acyl CoA: cholesterol acyltransferase is presented with a view to reflect upon the parametric requirement of various substitutions. (who.int)
Aminoimidazole1
- 5-amino-1-(5-phospho-D-ribosyl) imidazole-4-carboxylate is converted from aminoimidazole ribotide via phosphoribosylaminoimidazole carboxylase [EC: 4.1.1.21]. (ecmdb.ca)
Synthesis1
- A concise and highly efficient strategy for the synthesis of N-glycosyl imidazole analogues is reported. (ntu.edu.sg)
Amide1
- Tethering histamine to the C5 of the thymine base via an amide bond, allows the flexible positioning of the imidazole function in the major groove. (ugent.be)
Dimethyl1
- post-operative chemotherapy with dimethyl triazeno imidazole carboxamide and cisplatin was performed in some patients. (biomedcentral.com)
Inhibits1
- A mitochondria-targeted imidazole-substituted fatty acid inhibits cytochrome c peroxidase and mitigates radiation -induced death. (cdc.gov)
Interactions1
- The mutual interactions between the imidazole and the duplex and its influence on the imidazolium pKa(H) are investigated by placing a single modified thymine at four different positions in the center of the 14mer double helix. (ugent.be)
Resistance1
- View of Profile of the resistance to macrolides and imidazoles of Helicobacter pylori in a sample of the Portuguese population. (actamedicaportuguesa.com)
Protein1
- Given the ubiquitous participation of the histidine-based imidazole group in protein recognition and catalysis events, single histidine-like modified duplexes were investigated. (ugent.be)
Cells1
- Pyrrole-imidazole polyamide-mediated silencing of KCNQ1OT1 expression induces cell death in Wilms' tumor cells. (cdc.gov)
Products3
- https://www.selleckchem.com/products/imidazole-ket. (uchatoo.com)
- While 2,4-disubstituted imidazol-5-yl acetates are formed in the first case, 2,4-disubstituted imidazoles, bearing no substituent at position 5, are the products in the second case. (fiocruz.br)
- Any contraindication to imidazole products (known hypersensitivity to imidazoles). (who.int)
Cream2
- Luliconazole, an imidazole topical cream, is applied once daily for 2 weeks. (medscape.com)
- Imidazoles (clotrimazole or miconazole) can be applied overnight as a cream and used as a talc in powder form by day. (medassignments.com)
Acids2
- Identification of a pKa-regulating motif stabilizing imidazole-modified double-stranded DNA," NUCLEIC ACIDS RESEARCH , vol. 43, no. 1, pp. 51-62, 2015. (ugent.be)
- We designed and synthesized mitochondria-targeted triphenylphosphonium-conjugated imidazole-substituted oleic (TPP-OA) and stearic (TPP-SA) acids. (cdc.gov)
Clear1
- In conclusion, this is the first study demonstrating the potential of these new series of imidazoles to clear the systemic parasite burden in infected rats. (elsevier.com)
Type3
- Condensed Imidazoles of Type 5-5 with no Additional Heteroatom. (ellibs.com)
- Condensed Imidazoles of Type 5-5 with One Additional Heteroatom. (ellibs.com)
- Imidazole type ionic liquid--Shanghai Holdenchem CO.,Ltd. (holdenmaterial.com)
Intermediate2
- In contrast, the decomposition of the acetyl intermediate was remarkably accelerated (up to 10 3 -fold) by the introduction of the imidazole unit. (elsevier.com)
- 5-amino-1-(5-phospho-D-ribosyl) imidazole-4-carboxylate is an intermediate in purine metabolism. (ecmdb.ca)
Oral1
- Furthermore, a high selectivity index of imidazoles towards T. congolense in vitro and the oral LD 50 in rats support anti-parasite specific action. (elsevier.com)
Series2
- These two series of imidazoles, viz. (fiocruz.br)
- This study explored new series of imidazoles for antiTrypanosoma properties in vitro and in vivo. (elsevier.com)
Growth1
- The imidazoles showed moderate to strong and specific action against growth of T. congolense. (elsevier.com)
Cell2
- For both imidazole and pH based purifications the cell lysis should be done in buffered solution adjusted to pH 7.4, with sodium chloride supplemented up to 0.3 M. Following binding, a wash buffer with a pH of approximately 6.3 is recommended. (neb.com)
- Rabeprazole is an antisecretory drug (substituted Benz imidazole proton-pump inhibitor) that does not affect gastric acid secretion by blocking the gastric H+/ATPase (hydrogen-potassium adenosine triphosphates) at the secretory membrane of the gastric parietal cell. (visionpharmapk.com)
Unit1
- The acylation rate at the hydroxamate anion unit was affected only insignificantly by the presence of the imidazole unit, and was much more efficient than those at the imidazole site. (elsevier.com)
Presence3
- The presence of guanidinium cations permits cleavage at significantly higher temperatures than previously observed for DNAzymes with only amines and imidazoles. (ubc.ca)
- The presence of LiCl allows the convenient preparation of magnesiated imidazoles starting from unprotected iodoimidazoles. (elsevier.com)
- Kopp, F & Knochel, P 2007, ' Iodine-magnesium exchange on unprotected imidazoles in the presence of LiCl ', Synlett , no. 6, pp. 980-982. (elsevier.com)
Recommendations1
- What are the recommendations for pH based elution, as opposed to imidazole? (neb.com)
Study1
- Additionally, the in vivo study revealed that the imidazoles exhibited promising anti-Trypanosoma efficacy corroborating the in vitro anti-parasite capacity. (elsevier.com)