Tag: M.W=200-250

Tok, Fatih published the artcileSynthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors, HPLC of Formula: 61343-99-5, the main research area is monoamine oxidase cholinesterase inhibitor pyrazolone Schiff base preparation neurodegeneration; Acetylcholinesterase; Butyrylcholinesterase; Docking; Monoamine oxidase A; Monoamine oxidase B; Schiff base.

In the current work, Schiff base derivatives of antipyrine were synthesized. The chem. characterization of the compounds was confirmed using IR, 1H NMR, 13C NMR and mass spectroscopies. The inhibitory potency of synthesized compounds was investigated towards acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases A and B (MAO-A and MAO-B) enzymes. Some of the compounds displayed significant inhibitory activity against AChE and MAO-B enzymes, resp. According to AChE enzyme inhibition assay, compounds 3e and 3g were found as the most potent derivatives with IC50 values of 0.285 μM and 0.057 μM, resp. Also, compounds 3a (IC50 = 0.114 μM), 3h (IC50 = 0.049 μM), and 3i (IC50 = 0.054 μM) were the most active derivatives against MAO-B enzyme activity. To understand inhibition type, enzyme kinetics studies were carried out. Furthermore, mol. docking studies were performed to define and evaluate the interaction mechanism between compounds 3g and 3h and related enzymes. ADME (Absorption, Distribution, Metabolism, and Excretion) and BBB (Blood, Brain, Barrier) permeability predictions were applied to estimate pharmacokinetic profiles of synthesized compounds

Bioorganic Chemistry published new progress about Cholinesterase inhibitors (acetylcholinesterase, butyrylcholinesterase). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, HPLC of Formula: 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Leo, Pedro published the artcileA recyclable Cu-MOF-74 catalyst for the ligand-free O-arylation reaction of 4-nitrobenzaldehyde and phenol, Computed Properties of 61343-99-5, the main research area is reusable copper MOF catalyst arylation reaction green chem; nitrobenzenealdehyde phenol formyldiphenyl ether; 4-formyldiphenyl ether; 4-nitrobenzaldehyde; MOF; O-arylation reaction; catalyst; ligand-free; phenol; recyclable Cu-MOF-74.

The activity and recyclability of Cu-MOF-74 as a catalyst was studied for the ligand-free C-O cross-coupling reaction of 4-nitrobenzaldehyde (NB) with phenol (Ph) to form 4-formyldiphenyl ether (FDE). Cu-MOF-74 is characterized by having unsaturated copper sites in a highly porous metal-organic framework. The influence of solvent, reaction temperature, NB/Ph ratio, catalyst concentration, and basic agent (type and concentration) were evaluated. High conversions were achieved at 120°C, 5 mol % of catalyst, NB/Ph ratio of 1:2, DMF as solvent, and 1 equiv of K2CO3 base. The activity of Cu-MOF-74 material was higher than other ligand-free copper catalytic systems tested in this study. This catalyst was easily separated and reused in five successive runs, achieving a remarkable performance without significant porous framework degradation The leaching of copper species in the reaction medium was negligible. The O-arylation between NB and Ph took place only in the presence of Cu-MOF-74 material, being negligible without the solid catalyst. The catalytic advantages of using nanostructured Cu-MOF-74 catalyst were also proven.

Nanomaterials published new progress about Aromatic ethers Role: IMF (Industrial Manufacture), PREP (Preparation). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Computed Properties of 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kaplanek, Robert published the artcileFast and effective reduction of nitroarenes by sodium dithionite under PTC conditions: application in solid-phase synthesis, Synthetic Route of 35112-05-1, the main research area is nitroarene reduction aryl amine preparation solid phase synthesis; solid phase nitroarene reduction phase transfer catalyst.

Herein, conditions for the fast and effective reduction of aromatic nitro groups bound to hydrophobic polystyrene-based Wang and Rink resins utilizing sodium dithionite in dichloromethane-water under PTC conditions are reported. Tetrabutylammonium hydrogen sulfate (TBAHS) was found to be an effective phase-transfer catalyst for this reaction. This method allows for the reduction of nitro groups to amino groups under mild conditions with complete conversion and is tolerant of other functional groups. This method is a superior alternative to tin(II) chloride-based reduction, which is known for its shortcomings.

Tetrahedron Letters published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Synthetic Route of 35112-05-1.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Chen, Jiuxi published the artcileLigand-free copper-catalyzed O-arylation of nitroarenes with phenols, SDS of cas: 61343-99-5, the main research area is aryl ether preparation; nitroarene phenol arylation copper catalyst.

The first example of ligand-free copper-catalyzed O-arylation of nitroarenes with phenols was developed, achieving unsym. diaryl ethers in moderate to excellent yields. This arylation proceeded smoothly without promotion of the ligands, and displayed great functional group compatibility. Thus, the method represents a new, facile, and cost-effective approach to access unsym. diaryl ethers.

Tetrahedron published new progress about Aromatic ethers Role: SPN (Synthetic Preparation), PREP (Preparation). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, SDS of cas: 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Mooibroek, Tiddo J. published the artcileA threading receptor for polysaccharides, Safety of Pyrene-2-carboxylic acid, the main research area is receptor polysaccharide cellulose oligosaccharide monosaccharide preparation polypseudorotaxane chitosan.

Cellulose, chitin and related polysaccharides are key renewable sources of organic mols. and materials. However, poor solubility tends to hamper their exploitation. Synthetic receptors could aid dissolution provided they are capable of cooperative action, for example by multiple threading on a single polysaccharide mol. Here we report a synthetic receptor designed to form threaded complexes (polypseudorotaxanes) with these natural polymers. The receptor binds fragments of the polysaccharides in aqueous solution with high affinities (Ka up to 19,000 M-1), and is shown-by nuclear Overhauser effect spectroscopy-to adopt the threading geometry. Evidence from induced CD and at. force microscopy implies that the receptor also forms polypseudorotaxanes with cellulose and its polycationic analog chitosan. The results hold promise for polysaccharide solubilization under mild conditions, as well as for new approaches to the design of biol. active mols.

Nature Chemistry published new progress about Oligosaccharides Role: FMU (Formation, Unclassified), PRP (Properties), FORM (Formation, Nonpreparative). 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Safety of Pyrene-2-carboxylic acid.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Marino, Joseph P. published the artcileThe discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages, COA of Formula: C8H4ClF3O, the main research area is tertiary amine preparation reductive amination nucleophilic substitution; liver X receptor LXR agonist cholesterol efflux macrophage pharmacokinetics; structure activity coronary heart disease cholesterol homeostasis lipid metabolism.

The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism SAR studies around tertiary-amine lead mol. I, an LXR full agonist, revealed that steric and conformational changes to the acetic acid and propanolamine groups produce dramatic effects on agonist efficacy and potency. The new analogs possess good functional activity, demonstrating the ability to upregulate LXR target genes, as well as promote cholesterol efflux in macrophages.

Bioorganic & Medicinal Chemistry Letters published new progress about Liver X receptor β Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (agonists). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, COA of Formula: C8H4ClF3O.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Unsinn, Andreas published the artcileDirected Magnesiation of Polyhaloaromatics using the Tetramethylpiperidylmagnesium Reagents TMP2Mg.2LiCl and TMPMgCl.LiCl, COA of Formula: C9H8Cl2O2, the main research area is regioselective magnesium halo arene magnesium amide Grignard reagent preparation; chlorophenethylphenol antimicrobial natural product preparation.

A convenient and efficient functionalization of polyhaloaroms. via regioselective magnesiation has been developed. Starting from simple, inexpensive but structurally challenging arenes, metalation by magnesium amide bases was achieved under mild conditions. The desired Grignard reagents were stable towards aryne formation, were obtained in good yields within short reaction times and could be reacted with a variety of typical electrophiles, providing attractive, functionalized building blocks in good to excellent yields. As an application we have prepared the antimicrobial natural product 2,6-dichloro-3-phenethylphenol isolated from the New Zealand liverwort Riccardia marginata. This synthesis involves a mixed bimetallic compound prepared via metalation of a phenylboronic acid pinacol ester derivative and subsequent selective cross-coupling.

Advanced Synthesis & Catalysis published new progress about Amides Role: RGT (Reagent), RACT (Reactant or Reagent) (Mg amide magnesiation agents). 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, COA of Formula: C9H8Cl2O2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Safak, Cihat published the artcileSynthesis and Myorelaxant Activity of Fused 1,4-Dihydropyridines on Isolated Rabbit Gastric Fundus, Quality Control of 93118-03-7, the main research area is dihydropyridine derivative myorelaxant gastric fundus smooth muscle calcium channel.

Strategy, Management and Health PolicyEnabling Technol., Genomics, ProteomicsPreclin. ResearchPreclin. Development Toxicol., Formulation Drug Delivery, PharmacokineticsClin. Development Phases I-III Regulatory, Quality, ManufacturingPostmarketing Phase IV In the present study, 25 novel condensed 1,4-dihydropyridine (DHP) derivatives bearing cyclopentane, cyclohexane, or tetrahydrothiopene ring with a bulky and lipophilic moiety (3-pyridylmethyl) in the ester group were synthesized via a modified Hantzsch reaction, and their calcium channel modulator activities were assayed on isolated rabbit gastric fundus smooth muscle strips. To evaluate the myorelaxant effects of the compounds, the maximum relaxant response (Emax) and pD2 values were calculated The results indicated that all compounds produced concentration-dependent relaxation and the introduction of five- or six-membered rings to the DHP nucleus and 3-pyridiylmethyl moiety to the ester group led to potent calcium antagonists.

Drug Development Research published new progress about Calcium channels Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Quality Control of 93118-03-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wu, Hao published the artcileMicroarray-Assisted High-Throughput Identification of a Cell-Permeable Small-Molecule Binder of 14-3-3 Proteins, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is cell permeable peptide library preparation microarray screening protein binding.

The authors have used a small-mol. microarray (SMM) technique to identify cell-permeable small mol.-peptide hybrids that are capable of binding to all 14-3-3 proteins and thus inhibiting protein-protein interactions (PPI). Phosphoserine-containing peptide libraries were constructed on solid-phase using 243 different carboxylic acids for conjugation with N-terminus of individual peptides in one library, and 50 different amines for conjugation with C-terminus of individual peptides in the second library. For both libraries, biotin and GlyGly linkers were introduced at either N- or C-terminus of each peptide to facilitate subsequent immobilization onto avidin-functionalized glass slides. All the peptide conjugates were characterized by liquid chromatog./mass spectrometry and most were shown to be the correct mol. weight and of sufficient purity for direct microarray applications.

Angewandte Chemie, International Edition published new progress about 14-3-3 Proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kas’yan, L. I. published the artcile2-(1-Aminoethyl)bicyclo[2.2.1]heptane. Sulfonamides, ureas, and thioreas on its base, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is aminoethylbicycloheptane conformation electron density nucleophilic reactivity; sulfonamide aminoethylbicycloheptane preparation; urea aminoethylbicycloheptane preparation; thiourea aminoethylbicycloheptane preparation.

The known antiviral drug, 2-(1-aminoethyl)bicyclo[2.2.1]heptane, has been studied by mol. mechanics and quantum-chem. methods. The structure of both exo and endo isomers has been examined by the MMX procedure. Conformational compositions of the isomers and barriers to rotation about the C2-C8 bond have been compared with corresponding parameters of stereoisomeric 2-aminomethylbicyclo[2.2.1]heptanes which also exhibit antiviral activity. The electron d. distribution in the amines has been calculated by the semiempirical AM1 method, and their reactivity has been estimated on the basis of the calculated proton affinities and energies of localized MOs. Nucleophilic properties of the title compound have been studied in reactions with phenylmethane- and arenesulfonyl chlorides and alicyclic and aromatic isocyanates and isothiocyanates. The structure of sulfonamides, ureas, and thioureas thus obtained has been proved by IR and 1H spectroscopy.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about Amines Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent) (cage). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics