Day: October 13, 2022

Pflegr, Vaclav; Stepankova, Sarka; Svrckova, Katarina; Svarcova, Marketa; Vinsova, Jarmila; Kratky, Martin published the artcile< 5-Aryl-1,3,4-oxadiazol-2-amines Decorated with Long Alkyl and Their Analogues: Synthesis, Acetyl- and Butyrylcholinesterase Inhibition and Docking Study>, Application In Synthesis of 93-60-7, the main research area is aryloyl dodecyl oxadiazol amine preparation cholinesterase inhibition docking SAR; dodecyl aryloyl thiadiazol amine preparation acetyl butyrylcholinesterase inhibition docking; hydrazine carboxamide cyclization; 1,3,4-oxadiazole; 1,3,4-thiadiazole; acetylcholinesterase; butyrylcholinesterase; enzyme inhibition; molecular docking.

The compounds 5-aryl-1,3,4-oxadiazoles/thiadiazols decorated with dodecyl linked via nitrogen, sulfur or directly to this heterocycle I [R = Ph, 4-MeC6H4, 4-tBuC6H4, etc.,; X = O, S; Y = NH, S] was designed as potential inhibitors of AChE and BChE. Oxadiazoles/thiadiazols derivatives I were prepared from hydrazides by reaction with dodecyl isocyanate to form hydrazine-1-carboxamides II (yields 67-98%) followed by cyclization using p-toluenesulfonyl chloride and triethylamine in 41-100% yields. The derivatives I were screened for inhibition of AChE and BChE using Ellman’s spectrophotometric method. The compounds I showed a moderate dual inhibition with IC50 values of 12.8-99.2 for AChE and from 53.1μM for BChE. All the heterocycles I were more efficient inhibitors of AChE. The most potent inhibitor, N-dodecyl-5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine I [R =4-pyridyl, X= S, Y = NH] was subjected to advanced reversibility and type of inhibition evaluation. Structure-activity relationships of heterocycles I were identified. Many oxadiazoles I showed lower IC50 values against AChE than established drug rivastigmine. According to mol. docking, the compounds I interact non-covalently with AChE and BChE and block entry into enzyme gorge and catalytic site, resp.

Pharmaceuticals published new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Application In Synthesis of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Talik, Tadeusz; Talik, Zofia published the artcile< 2-Fluoronitro-derivatives of pyridine and picolines>, Name: 2-Fluoro-6-methyl-3-nitropyridine, the main research area is pyridine fluoro nitro; picoline fluoro nitro; diazotization aminopyridine.

6-Fluoro derivatives from 4-nitro- and 3,5- and 3,4-dinitropyridine, 3- and 5-nitro- and 3,5-dinitro-4-picoline, 3- and 5-nitro- and 3,5-dinitro-2-picoline, and 5-nitro-3-picoline as well as 2-fluoro-5-nitro-3-picoline were prepared in 52.5-85% yields by diazotization of the corresponding amino derivatives in 65% HF.

Roczniki Chemii published new progress about 19346-45-3. 19346-45-3 belongs to class pyridine-derivatives, and the molecular formula is C6H5FN2O2, Name: 2-Fluoro-6-methyl-3-nitropyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Barone, Antonella; Cristiano, Maria Chiara; Cilurzo, Felisa; Locatelli, Marcello; Iannotta, Dalila; Di Marzio, Luisa; Celia, Christian; Paolino, Donatella published the artcile< Ammonium glycyrrhizate skin delivery from ultradeformable liposomes: A novel use as an anti-inflammatory agent in topical drug delivery>, Safety of 3-(Methoxycarbonyl)pyridine, the main research area is ammonium glycyrrhizate skin drug delivery antiinflammatory activity; Ammonium glycyrrhizate; Anti-inflammatory activity; Colloidal nanocarriers; Topical administration; Ultradeformable liposomes.

Although several nanoformulations, such as ethosomes, are designed to provide a systemic effect through a topical application, there are different limitations to the distribution inside the blood stream. For this reason, ultradeformable liposomes, or transfersomes, are selected to improve the topical delivery of drugs and allow the distribution of payloads in the blood stream because they pass intact through the stratum corneum epidermis barrier, due to the presence of sodium cholate, aqueous cutaneous gradient, and the rapid penetration of transfersomes by cutaneous tight junctions, thus allowing the systemic delivery of different therapeutic cargo in non-occlusive conditions. The aim of this work was the synthesis and physicochem. characterization of the ammonium glycyrrhizinate-loaded ultradeformable liposomes, the evaluation of drug release and permeation through stratum corneum and epidermis barrier. The in vivo anti-inflammatory effect of ammonium glycyrrhizinate-loaded ultradeformable liposomes was tested on human healthy volunteers. The results demonstrated that the ammonium glycyrrhizinate-loaded ultradeformable liposomes decreased the skin inflammation on the human volunteers and the resulting nanoformulations can be used as a potential topical drug delivery system for anti-inflammatory therapy.Parts of these results were presented as a poster communication at the Recent Developments in Pharmaceutical Anal. 2019 (RDPA 2019), Chieti, Italy.

Colloids and Surfaces, B: Biointerfaces published new progress about Anti-inflammatory agents. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Safety of 3-(Methoxycarbonyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Oka, Naoki; Yamada, Tsuyoshi; Sajiki, Hironao; Akai, Shuji; Ikawa, Takashi published the artcile< Aryl Boronic Esters Are Stable on Silica Gel and Reactive under Suzuki-Miyaura Coupling Conditions>, Category: pyridine-derivatives, the main research area is aryl boronic ester bromoarene palladium Suzuki Miyaura coupling; biaryl preparation.

A wide range of aryl boronic 1,1,2,2-tetraethylethylene glycol esters [ArB(Epin)s] were readily synthesized. Purifying aryl boronic esters by conventional silica gel chromatog. is generally challenging; however, these introduced derivatives were easily purified on silica gel and isolated in excellent yields. The purified ArB(Epin) was subjected to Suzuki-Miyaura couplings, which provided higher yields of the desired biaryl products than those obtained using the corresponding aryl boronic acids or pinacol esters.

Organic Letters published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Grozavu, Alexandru; Hepburn, Hamish B.; Smith, Philip J.; Potukuchi, Harish K.; Lindsay-Scott, Peter J.; Donohoe, Timothy J. published the artcile< The reductive C3 functionalization of pyridinium and quinolinium salts through iridium-catalysed interrupted transfer hydrogenation>, COA of Formula: C7H7NO2, the main research area is pyridinium salt formaldehyde iridium catalyst regioselective reductive hydroxymethylation; quinolinium salt formaldehyde iridium catalyst regioselective reductive hydroxymethylation; tetrahydropyridine preparation; tetrahydroquinoline preparation.

Aromatic rings are ubiquitous in organic chem. and form the basis of many com. products. Despite the numerous routes available for the preparation of aromatic compounds, there remain few methods that allow their conversion into synthetically useful partially saturated derivatives and even fewer that allow new C-C bonds to be formed at the same time. Here we set out to address this problem and uncover a unique catalytic partial reduction reaction that forms partially saturated azaheterocycles from aromatic precursors. In this reaction, methanol and formaldehyde are used for the reductive functionalization of pyridines and quinolines using catalytic iridium; thus, inexpensive and renewable feedstocks are utilized in the formation of complex N-heterocycles. By harnessing the formation of a nucleophilic enamine intermediate, the C-C bond-forming process reverses the normal pattern of reactivity and allows access to the C3 position of the arene. Mechanistic investigations using D-labeling experiments reveal the source of hydride added to the ring and show the reversible nature of the iridium-hydride addition

Nature Chemistry published new progress about C-C bond formation. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, COA of Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jevremovic, Anka; Bozinovic, Nevena; Arsenijevic, Dragana; Marmakov, Sanal; Nedic Vasiljevic, Bojana; Uskokovic-Markovic, Snezana; Bajuk-Bogdanovic, Danica; Milojevic-Rakic, Maja published the artcile< Modulation of cytotoxicity by consecutive adsorption of tannic acid and pesticides on surfactant functionalized zeolites>, Formula: C21H38ClN, the main research area is tannic acid pesticide zeolite adsorption cytotoxicity.

This study investigated the environmental application of FAU type zeolites modified with cationic surfactants (cetylpyridinium chloride, tetrapropylammonium chloride and benzalkonium chloride). Adsorbent characterization was conducted using Fourier-transform IR and Raman spectroscopy, thermogravimetry and DTA, at. force microscopy and X-ray powder diffraction. The efficiency for tannic acid adsorption from aqueous solution on the surface of prepared composites is studied and the adsorption process was modelled with different isotherm equations. Surfactant modifications of zeolites led to improved adsorption properties compared to FAU zeolites alone. The proposed mechanism controlling the adsorption of tannic acid onto surfactant modified zeolites mainly relies on π-π and hydrophobic interactions. The investigated materials are promising adsorbents for tannic acid and similar phenolics and may be important for environmental and dietary aspects of polyphenol persistence and usage. Further on, functionalized zeolites were studied for insecticide acetamiprid removal, prior to and after tannic acid retention. Promising findings of insecticide co-adsorption with tannic acid led to cytotoxicity evaluation. The cytotoxicity modulation effect of zeolites and tannic acid on acetamiprid points to the essential role of both components in insecticide toxicity reduction

Environmental Science: Processes & Impacts published new progress about Adsorption. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Formula: C21H38ClN.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bratt, Jack; Iddon, Brian; Mack, Arthur G.; Suschitzky, Hans; Taylor, Jack A.; Wakefield, Basil J. published the artcile< Polyhaloaromatic compounds. Part 41. Photochemical dehalogenation and arylation reactions of polyhaloaromatic and polyhaloheteroaromatic compounds>, Recommanded Product: 2,3,4,6-Tetrachloropyridine, the main research area is photochem dehalogenation arylation haloarom compound; photocyclization thiopyridine; halobenzene poly photochem dehalogenation arylation; pyridine halo dehalogenation arylation.

Photolysis of pentachloro- and pentabromopyridine in Et2O led to β-halogen loss and the formation of a product of attack by Et2O, I (R = Cl, Br, resp.). Both 4-bromo- and 4-iodotetrachloropyridines underwent exclusive loss of Br and iodine, resp. Perhalothiophenes, tetrachloropyrimidine and C6Cl6 underwent similar dehalogenation reactions. Photolysis of C6Cl5I (II), tetrachloroiodopyridines and trichloro-5-iodothiophene in C6H6 gave the corresponding polychloroaryl- or polychloroheteroarylbenzenes. E.g., II underwent photolysis in C6H6 to give 95% 2,3,4,5,6-pentachlorobiphenyl. Photolysis of the pyridines III (R1 = SPh, SC6Cl5) gave the corresponding photocyclization products IV (R2 = H, Cl) resp.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about Photochemical arylation. 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Recommanded Product: 2,3,4,6-Tetrachloropyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lee, Johnny Ching-Wei; Porcar, Lionel; Rogers, Simon A. published the artcile< Unveiling temporal nonlinear structure-rheology relationships under dynamic shearing>, COA of Formula: C21H38ClN, the main research area is micelle nonlinear rheol dynamic shearing; LAOS; nonlinear rheology; polymer rheology; rheo SANS; structure–rheology relationship; viscoelastic; worm-like micelles.

Understanding how microscopic rearrangements manifest in macroscopic flow responses is one of the central goals of nonlinear rheol. studies. Using the sequence-of-phys.-processes framework, we present a natural 3D structure-rheol. space that temporally correlates the structural and nonlinear viscoelastic parameters. Exploiting the rheo-small-angle neutron scattering (rheo-SANS) techniques, we demonstrate the use of the framework with a model system of polymer-like micelles (PLMs), where we unveil a sequence of microscopic events that micelles experience under dynamic shearing across a range of frequencies. The least-aligned state of the PLMs is observed to migrate from the total strain extreme toward zero strain with increasing frequency. Our proposed 3D space is generic, and can be equally applied to other soft materials under any sort of deformation, such as startup shear or uniaxial extension. This work therefore provides a natural approach for researchers to study complex out-of-equilibrium structure-rheol. relationships of soft materials.

Polymers (Basel, Switzerland) published new progress about Linear viscoelasticity. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, COA of Formula: C21H38ClN.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Grabner, Sabina; Modec, Barbara published the artcile< Zn(II) curcuminate complexes with 2,2′-bipyridine and carboxylates>, Recommanded Product: 2,2′-Bipyridine, the main research area is Zn(II) complexes; crystal structures; curcumin; stability.

Two novel zinc(II) compounds with curcuminate (abbreviated as cur-), [Zn(CH3COO)(cur)(bpy)] (1)·CH3OH·2H2O (bpy = 2,2′-bipyridine) and [Zn(PhCOO)(cur)(bpy)] (2)·CH3OH, have been synthesized and characterized. Their composition has been determined by single-crystal X-ray structure anal. Complexes 1 and 2 are similar: in both a five-fold coordination environment of zinc(II) consists of a monodentate carboxylate, a chelating bidentate 2,2′-bipyridine, and curcuminate, which is bound via a deprotonated 1,3-dione moiety. In 1, 2,2′-bipyridine nitrogen atoms and curcuminate oxygen atoms form the base of a square pyramid, whereas the acetate oxygen occupies its apex. The O3N2 donor set in 2 defines a polyhedron which more closely resembles a trigonal bipyramid. The packing in the crystal lattices of both compounds is governed by hydrogen-bonds. Complexes 1 and 2 display higher stability than curcumin in buffered media at pH = 7.0, however, the degradation of coordinated cur- is comparable to that of yellow pigment curcumin (curH) when the pH is raised to 7.2. Both complexes 1 and 2 in DMSO exhibit fluorescence with Stokes shifts of 5367 and 4634 cm-1, resp.

Molecules published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Recommanded Product: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Jun-Xia; Du, Zhong-Xiang; Pan, Qiu-Yue; Zhang, Lu-Lu; Liu, Duo-Li published the artcile< The first 3,5,6-trichloropyridine-2-oxyacetate bridged manganese coordination polymer with features of π···π stacking and halogen···halogen interactions: Synthesis, crystal analysis and magnetic properties>, Electric Literature of 366-18-7, the main research area is trichloropyridineoxyacetate bridged manganese bipyridine coordination polymer preparation crystal structure; pi stacking halogen interaction crystal structure magnetic property manganese.

A new coordination polymer [Mn(3,5,6-tcpa)2(2,2′-bipy)]n (1) has been synthesized by the hydrothermal reaction of manganese sulfate hydrate with 3,5,6-trichloropyridine-2-oxyacetic acid (3,5,6-Htcpa) and 2,2′-bipyridine (2,2′-bipy) coligands. The x-ray single-crystal diffraction anal. shows that the MnII center is in deformed octahedral geometry bonded by two pyridyl nitrogen atoms of 2,2′-bipy mol. and four carboxy oxygen atoms of four different 3,5,6-tcpa- ligands. The 3,5,6-tcpa- anions play as bidentate bridging-μ2 linkers and connect neighboring MnII ions together to form the 1D double-stranded chain structure of 1, which displays interesting chair form [Mn2(COO)2] eight-membered rings. 1 Is further assembled into 3D network by the co-effects of π···π stacking and Cl···Cl halogen bonds interactions. In addition, the magnetic characterizations indicated weak antiferromagnetic coupling between MnII centers for 1.

Inorganica Chimica Acta published new progress about Antiferromagnetic exchange. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Electric Literature of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem