Category: imidazoles-derivatives

Elsheikh, A. A.; Braun, L. J.; Mansour, S. M. G.; Orabi, A.; Alqahtani, A. S.; Benfield, D. A.; Chase, C. C. L. published the artcile< The effect of human interferon alpha on replication of different bovine viral diarrhea virus strains>, Formula: C5H5N5, the main research area is interferon alpha bovine viral diarrhea virus replication.

In the present study, we evaluated the comparative effect of exogenous human IFN-α (HuIFN-α) on different BVDV biotypes and genotypes. The results showed that exogenous HuIFN-α greatly inhibited the growth of different BVDV biotypes and genotypes. However, HuINF-α has a significant inhibitory effect on cp biotype compared to ncp one without significant variation between different genotypes. The effect of HuIFN-α on BVDV reached the maximum level at early stages of infection (0-20 h post infection) and increased in a dose-dependent manner (10-500 U/mL). Quant. realtime RT-PCR was used to evaluate the effect of exogenous HuIFN-α on RNA synthesis of both BVDV biotypes. HuIFN-α reduced RNA production of cp by 4 logs compared to only 2 logs for ncp strains. Addnl., the antiviral effect of IFN-α against both BVDV biotypes seems to be independent of the RNA-dependent protein kinase (PKR) activation as assayed by direct anal. of in vivo phosphorylation of eIF2-α and by 2-aminopurine (2-AP) treatment. Collectively, these results indicated that the exogenous HuIFN-α treatment has an inhibitory effect not only on cp BVDV biotype but also on the ncp BVDV. The antiviral effect of exogenous HuIFN-α was biotype, time, dose but not genotype dependent. PKR has no role in the inhibitory effect suggesting that other IFN-antiviral pathways were involved.

Acta Virologica (English Edition) published new progress about Bovine diarrhea virus. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Formula: C5H5N5.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Klein, Hannah L.; Ang, Kenny K. H.; Arkin, Michelle R.; Beckwitt, Emily C.; Chang, Yi-Hsuan; Fan, Jun; Kwon, Youngho; Morten, Michael J.; Mukherjee, Sucheta; Pambos, Oliver J.; el Sayyed, Hafez; Thrall, Elizabeth S.; Vieira-da-Rocha, Joao P.; Wang, Quan; Wang, Shuang; Yeh, Hsin-Yi; Biteen, Julie S.; Chi, Peter; Heyer, Wolf-Dietrich; Kapanidis, Achillefs N.; Loparo, Joseph J.; Strick, Terence R.; Sung, Patrick; Van Houten, Bennett; Niu, Hengyao; Rothenberg, Eli published the artcile< Guidelines for DNA recombination and repair studies: mechanistic assays of DNA repair processes>, Category: imidazoles-derivatives, the main research area is aminopurine DNA recombination repair mutagenesis review; DNA breaks; DNA helicases; DNA repair centers; DNA repair synthesis; DNA resection; DSBs; FRET; PALM; chromatin dynamics; chromosome rearrangements; crossovers; double strand break repair; endonuclease protection assay; fluorescent proteins; genome instability; gross chromosome rearrangements; homologous recombination; mismatch repair; nonhomologous end joining; nucleotide excision repair; photoactivated fluorescent proteins; recombinase filament assembly; single-molecule; single-particle tracking; structure-selective endonucleases; super resolution; synthesis-dependent strand annealing; transcription coupled repair.

A review. Genomes are constantly in flux, undergoing changes due to recombination, repair and mutagenesis. In vivo, many of such changes are studies using reporters for specific types of changes, or through cytol. studies that detect changes at the single-cell level. Single mol. assays, which are reviewed here, can detect transient intermediates and dynamics of events. Biochem. assays allow detailed investigation of the DNA and protein activities of each step in a repair, recombination or mutagenesis event. Each type of assay is a powerful tool but each comes with its particular advantages and limitations. Here the most commonly used assays are reviewed, discussed, and presented as the guidelines for future studies.

Microbial Cell published new progress about DNA repair. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Salvitti, Chiara; Bortolami, Martina; Chiarotto, Isabella; Troiani, Anna; de Petris, Giulia published the artcile< The Knoevenagel condensation catalysed by ionic liquids: a mass spectrometric insight into the reaction mechanism>, HPLC of Formula: 700370-07-6, the main research area is anisaldehyde cyanoacetate methylimidazolium chloride Knoevenagel condensation mechanism.

The creation of carbon-carbon bonds is still a highly required topic in organic chem. for the capacity to give a wide variety of new products of industrial value. Accordingly, the Knoevenagel condensation between activated methylene compounds and aldehydes is one of the most known carbon coupling reactions. In this work, the catalytic activity of imidazolium-based ionic liquids (1-butyl-3-methylimidazolium acetate, 1-butyl-3-methylimidazolium chloride, 1-methyl-3-carboxymethylimidazolium chloride) was studied under solvent-free conditions and compared with that of sodium salts (sodium chloride, sodium acetate). Mass spectrometric techniques were used to monitor the formation of the reaction products and to detect the key intermediates of the process. Based on the catalyst employed different reaction mechanisms were highlighted, thus laying the foundation for the design of more specific and efficient catalysts.

New Journal of Chemistry published new progress about Electrospray ionization mass spectrometry. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, HPLC of Formula: 700370-07-6.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

G-Dayanandan, Narendran; Scocchera, Eric W.; Keshipeddy, Santosh; Jones, Heather F.; Anderson, Amy C.; Wright, Dennis L. published the artcile< Direct Substitution of Arylalkynyl Carbinols Provides Access to Diverse Terminal Acetylene Building Blocks>, Electric Literature of 1003-21-0, the main research area is aryl propyne preparation reduction substitution arylalkynyl carbinol.

To develop next generation antifolates for the treatment of trimethoprim-resistant bacteria, synthetic methods were needed to prepare a diverse array of 3-aryl-propynes with various substitutions at the propargyl position. A direct route was sought whereby nucleophilic addition of acetylene to aryl carboxaldehydes would be followed by reduction or substitution of the resulting propargyl alc. The direct reduction, methylation, and dimethylation of these readily available alcs. provide efficient access to this uncommon functional array. In addition, an unusual silane exchange reaction was observed in the reduction of the propargylic alcs.

Organic Letters published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Electric Literature of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Mergehenn, R.; Haase, W.; Allmann, R. published the artcile< Crystal structures of chloro- and γ-bromo-(2-dibutylaminoethanolato)copper(II)>, Related Products of 1003-21-0, the main research area is mol structure copper aminoethanolato halo; chloro copper aminoethanolato structure; bromo copper aminoethanolato structure.

Addnl. data considered in abstracting and indexing are available from a source cited in the original document. The crystal structures of halo-(2-dibutylaminoethanolato)copper(II) [(C10H22NOCuX)4, X = Cl (I), Br (II) were determined by single-crystal x-ray diffractometer methods using 4331 and 3915 independent reflections, resp., from 3-dimensional diffractometer data (Mo Ka radiation). The isomorphous compounds belong to space group P1̅ with a 15·563(10), b 16·280(11), c 11·659(8) Å, α 93·49(10), β 100·32(10), γ 112·51(10)° for I and a 15·539(10), b 16·452(11), c 11·766(8) Å, α 94·58(10), β 100·65(10), γ 111·67(10)° for II. The structures were refined by least-squares methods to final residuals of 0.084 and 0.071, resp. The tetrameric clusters of cubane-type mol. structures have mean Cu-Cu separations of 3·240(3) and 3·268(3) Å. The Cu coordination is distorted square pyramidal with Cu bonded to 3 O, 1N, and 1 halogen. The distance to the apical O is longer than to the other 2 O. The average bond lengths are Cu-O 1·9778) and 1·963(10) Å (short Cu-O separations), Cu-O 2·424(8) and 2·480(10) Å (long-Cu-O separations), Cu-N 2·054(11) and 2·066(13) Å, and Cu-hal 2·234(4) and 2·382(3) Å.

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry published new progress about Crystal structure. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Related Products of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wang, Mo; Zhang, Zhenfeng; Xie, Fang; Zhang, Wanbin published the artcile< Cu-catalyzed amidation of halogenated imidazoles>, Reference of 1003-21-0, the main research area is imidazole halo amide cyclic copper amidation catalyst; amido imidazole preparation; amide cyclic heterocycle halo copper amidation catalyst; heterocycle amido preparation.

An efficient methodol. involving the Cu-catalyzed amidation of halogenated imidazoles has been successfully developed. The amidated product of 5-bromo-1-alkylimidazole was further applied to the synthesis of a new chiral imidazole nucleophilic catalyst for the kinetic resolution of secondary alcs.

Chemical Communications (Cambridge, United Kingdom) published new progress about Amidation. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Reference of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Figuera-Losada, Mariana; Stathis, Marigo; Dorskind, Joelle M.; Thomas, Ajit G.; Bandaru, Veera Venkata Ratnam; Yoo, Seung-Wan; Westwood, Nicholas J.; Rogers, Graeme W.; McArthur, Justin C.; Haughey, Norman J.; Slusher, Barbara S.; Rojas, Camilo published the artcile< Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties>, Application In Synthesis of 6823-69-4, the main research area is neurodegeneration cambinol sphingomyelinase 2 ceramide.

Ceramide is a bioactive lipid that plays an important role in stress responses leading to apoptosis, cell growth arrest and differentiation. Ceramide production is due in part to sphingomyelin hydrolysis by sphingomyelinases. In brain, neutral sphingomyelinase 2 (nSMase2) is expressed in neurons and increases in its activity and expression have been associated with pro-inflammatory conditions observed in Alzheimer’s disease, multiple sclerosis and human immunodeficiency virus (HIV-1) patients. Increased nSMase2 activity translates into higher ceramide levels and neuronal cell death, which can be prevented by chem. or genetic inhibition of nSMase2 activity or expression. However, to date, there are no soluble, specific and potent small mol. inhibitor tool compounds for in vivo studies or as a starting point for medicinal chem. optimization. Moreover, the majority of the known inhibitors were identified using bacterial, bovine or rat nSMase2. In an attempt to identify new inhibitor scaffolds, two activity assays were optimized as screening platform using the recombinant human enzyme. First, active hits were identified using a fluorescence-based high throughput compatible assay. Then, hits were confirmed using a 14C sphingomyelin-based direct activity assay. Pharmacol. active compounds and approved drugs were screened using this strategy which led to the identification of cambinol as a novel uncompetitive nSMase2 inhibitor (Ki = 7 μM). The inhibitory activity of cambinol for nSMase2 was approx. 10-fold more potent than for its previously known target, silence information regulator 1 and 2 (SIRT1/2). Cambinol decreased tumor necrosis factor-α or interleukin-1 β-induced increases of ceramide and cell death in primary neurons. A preliminary study of cambinol structure and activity allowed the identification of the main structural features required for nSMase2 inhibition. Cambinol and its analogs may be useful as nSMase2 inhibitor tool compounds to prevent ceramide-dependent neurodegeneration.

PLoS One published new progress about Alzheimer disease. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Application In Synthesis of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Iida, Hiroki; Umebayashi, Naofumi; Yashima, Eiji published the artcile< Photoswitchable organocatalysis in acylation of alcohol using dithienylethene-linked azoles>, SDS of cas: 1003-21-0, the main research area is dithienylethene linked azole preparation photoswitchable organocatalyst acylation alc.

Three novel dithienylethenes bearing azole derivatives were synthesized and found to undergo reversible photocyclization of the dithienylethene units upon alternate irradiation with UV and visible light. Among them, the dithienylethene-linked imidazole and N-phenylimidazole exhibited a relatively high organocatalytic activity for the acylation of 2-decanol with acetic anhydride, and the catalytic activity of the dithienylethene-linked imidazole could be switched by reversible photoinduced cyclization/cycloreversion of the dithienylethene unit.

Tetrahedron published new progress about Acylation. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, SDS of cas: 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kladova, O. A.; Kuznetsova, A. A.; Barthes, Nicolas P. F.; Michel, Benoit Y.; Burger, Alain; Fedorova, O. S.; Kuznetsov, N. A. published the artcile< New Fluorescent Analogs of Nucleotides Based on 3-Hydroxychromone for Recording Conformational Changes of DNA>, Formula: C5H5N5, the main research area is hydroxychromone fluorescence quenching DNA conformational change.

It has recently been found that derivatives of nucleotides containing a 3-hydroxychromone fluorescent dye can be used as sensitive markers of conformational changes of DNA. In this work, a comparative anal. of two fluorescent nucleotide derivatives-3-hydroxychromone a (3HC) and 3HC-modified uridine (FCU)-was performed during the study of protein-nucleic acid interactions for several human DNA repair enzymes, removing damaged nucleotides: DNA glycosylases AAG, OGG1, UNG2, and MBD4 and AP endonuclease APE1. The changes of fluorescence intensity significantly depended on the nature of neighbor nucleotides and may be opposite in direction for different cases. The FCU residue located in the complementary strand opposite to damaged nucleotide or in the same strand moved by few nucleotides, is very sensitive to processes induced by DNA glycosylases in the course of formation of enzyme-substrate complexes, which include local melting and bending of the DNA chain, as well as eversion of the damaged nucleotide from DNA double helix and insertion of amino acids of the active site into the void.

Russian Journal of Bioorganic Chemistry published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Formula: C5H5N5.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Garbaccio, Robert M.; Brnardic, Edward J.; Fraley, Mark E.; Hartman, George D.; Hutson, Pete H.; O’Brien, Julie A.; Magliaro, Brian C.; Uslaner, Jason M.; Huszar, Sarah L.; Fillgrove, Kerry L.; Small, James H.; Tang, Cuyue; Kuo, Yuhsin; Jacobson, Marlene A. published the artcile< Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor>, Product Details of C8H4ClN3, the main research area is oxazolo benzimidazole derivative preparation allosteric modulator mGluR2 receptor antipsychotic; GPCR; Oxazolobenzimidazoles; allosteric modulators; hyperlocomotion model; metabotropic glutamate 2 receptor; schizophrenia.

Novel oxazolobenzimidazoles are described as potent and selective pos. allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its phys. and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clin. antipsychotic treatments for schizophrenia.

ACS Medicinal Chemistry Letters published new progress about Antipsychotics. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Product Details of C8H4ClN3.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem