Month: November 2022

Faul, Margaret M. published the artcileAcyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ, Product Details of C18H24N2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2003), 13(11), 1857-1859, database is CAplus and MEDLINE.

The synthesis and structure-activity relationship (SAR) trends of a new class of N-(azacycloalkyl)bisindolylmaleimides, e.g. I (R¹ = CH₂-pyridyl, R² = Me, n = 2), acyclic derivatives of staurosporine, is described. I exhibits an IC₅₀ of 40-50 nM against the human PKCβ₁ and PKCβ₂ isoenzymes and selectively inhibits the PKCβ isoenzymes in comparison to other PKC isoenzymes (α, γ, δ, ε, λ, and η). The series is also kinase selective for PKC in comparison to other ATP-dependent kinases. A comparison of the protein kinase C (PKC) isoenzyme and kinase activity of the series is made to the kinase inhibitor staurosporine.

Bioorganic & Medicinal Chemistry Letters published new progress about 170364-89-3. 170364-89-3 belongs to piperidines, auxiliary class Indole,Piperidine,Amide, name is tert-Butyl 4-(1H-indol-1-yl)piperidine-1-carboxylate, and the molecular formula is C18H24N2O2, Product Details of C18H24N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Fidecka, Katarzyna published the artcileQuantification of amino groups on halloysite surfaces using the Fmoc-method, Category: piperidines, the publication is RSC Advances (2020), 10(24), 13944-13948, database is CAplus and MEDLINE.

The functionalization of halloysite nanotube (HNT) surfaces with aminosilanes is an important strategy for their further decoration with organic mols. to obtain hybrid inorganic-organic nanoarchitectures to be used in catalysis and drug delivery. The exact quantification of amino groups on the surface is an important aspect in view of the obtainment of systems with a known number of loaded mols. In the present study, we describe a simple and reliable method for the correct quantification of groups present on HNT surfaces after their reaction with aminopropyltriethoxysilane (APTES). This method, applied for the first time to HNT chem., was based on the use of Fmoc groups as probes covalently bound to APTES and quantified by UV-Vis after release from the HNT-APTES-Fmoc system. Interestingly, this method showed great accordance with the already employed quant. thermogravimetric anal. (TGA), with some benefits such as simple and non-destructive procedure, besides the possibility to monitor the deprotection reaction.

RSC Advances published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C19H21N, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Mukherjee, Mana Mohan published the artcileSynthetic Routes toward Acidic Pentasaccharide Related to the O-Antigen of E. coli 120 Using One-Pot Sequential Glycosylation Reactions, Recommanded Product: 1-(Phenylsulfinyl)piperidine, the publication is Journal of Organic Chemistry (2017), 82(11), 5751-5760, database is CAplus and MEDLINE.

Concise syntheses of the acidic pentasaccharide, related to the O-antigenic polysaccharide of Escherichia coli 120, as its p-methoxyphenyl glycoside, have been achieved using a one-pot sequential glycosylation technique. The glycosylation have been accomplished either by the activation of the thioglycosides using NIS in the presence of FeCl₃ or by a pre-activation by Ph₂SO, TTBP, Tf₂O, and the activation of the trichloroacetimidates using FeCl₃ alone or TMSOTf. Most of the intermediate steps are high yielding, and the stereo outcomes of the glycosylation steps were excellent. The syntheses of the targeted pentasaccharide have been performed with both three- and four-component, one-pot sequential glycosylation reactions, and in both cases, the orthogonal glycosylation is carried out utilizing catalytic activity of FeCl₃. A late-stage TEMPO-mediated regioselective oxidation has been performed to achieve the required uronic acid motif.

Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Recommanded Product: 1-(Phenylsulfinyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Ullrich, Thomas published the artcileSynthesis and immobilization of erythro-C14-ω-aminosphingosine-1-phosphate as a potential tool for affinity chromatography, Recommanded Product: 1-((9H-Fluoren-9-yl)methyl)piperidine, the publication is ChemMedChem (2008), 3(2), 356-360, database is CAplus and MEDLINE.

A sphingosine-1-phosphate (S1P) analog containing a terminal alkyl chain amino group is synthesized in a few steps via olefin cross-metathesis of an optically resolved intermediate and subsequent phosphorylation. Regioselective acylation of this intermediate at its N terminus in solution is demonstrated as a model reaction and provides a biol. active derivative Finally, the ω-amino intermediate is immobilized on an affinity matrix. The choice of a UV-active phosphate protecting group allows for quantification of resin loading after cleavage which amounted to 66%.

ChemMedChem published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C13H22BN3O4, Recommanded Product: 1-((9H-Fluoren-9-yl)methyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Haake, M. published the artcileDialkylaminosuccinimidosulfonium compounds. 3. A simple method for the oxidation of sulfenamides to sulfinamides, Safety of 1-(Phenylsulfinyl)piperidine, the publication is Synthesis (1979), 97, database is CAplus.

R¹SNR₂ were oxidized by treatment with N-chlorosuccinimide in CH₂Cl₂ to give a succinimidosulfonium chloride intermediate which was hydrolyzed in situ by aqueous KHCO₃ to give 41-85% R¹SONR₂ [R₂ = Me₂, (CH₂)₅, or (CH₂)₂O(CH₂)₂; R¹ = Et or Ph].

Synthesis published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Safety of 1-(Phenylsulfinyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wang, Gen published the artcileActivation of peroxydisulfate by defect-rich CuO nanoparticles supported on layered MgO for organic pollutants degradation: An electron transfer mechanism, Quality Control of 826-36-8, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2022), 431(Part_1), 134026, database is CAplus.

Heterogeneous activation of peroxydisulfate (PDS) by transition metal oxides offers a promising strategy for organic pollutants removal but suffers from low electron transfer efficiency. Herein, layered MgO supported CuO nanoparticles was prepared by thermal conversion of metal-phenolic networks of Cu²⁺/Mg²⁺ and tannic acid. CuO nanoparticles (â‰? nm) were spatial monodispersed on layered MgO, inducing the formation of electron deficient Cu³⁺ and surface oxygen vacancies and thus facilitated adsorption and activation of PDS. The electron-rich CuO/MgO hybrid catalysts manifested good catalytic performance of PDS activation for organic pollutants removal. At 0.18 g/L of CuO/MgO hybrid catalyst and 0.2 mM of PDS, complete removal of bisphenol A (BPA) was achieved with a high kinetic constant (0.1 min^-1, 50 min). Quenching experiments, ESR tests, PDS decomposition behaviors, electrochem. anal. and in situ ATR-FTIR and Raman spectroscopy revealed a nonradical pathway of electron transfer for PDS activation. The CuO/MgO hybrid catalysts exhibited wide working pH range from 3 to 11, selective oxidation capability, good resistance to halide ion and high utilization efficiency of PDS, and thus would be a promising candidate for wastewater remediation.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C5H5ClIN, Quality Control of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Thomas, Aleena published the artcileTrichloroacetic acid fueled practical amine purifications, Quality Control of 826-36-8, the publication is Beilstein Journal of Organic Chemistry (2022), 225-231, database is CAplus and MEDLINE.

On out of equilibrium mol. machinery, using trichloroacetic acid (TCA), disclosed a purification technique considerably decreasing the number of operations and the waste generation required for such purifications. At first, TCA triggered the precipitation of the amines through their protonated salt formation, enabling the separation with the impurities. From these amine salts, simple decarboxylation of TCA liberated volatile CO₂ and chloroform afforded directly the pure amines. Through this approach, a broad range of diversely substituted amines were isolated with success.

Beilstein Journal of Organic Chemistry published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C13H26N2, Quality Control of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Nadaf, AfraQuasar A. published the artcileSynthesis of N-(4-(6-chloro-imidazo[1,2-a]pyridin-2-yl)phenyl) Acetamide Derivatives as Antitubercular Agents, Quality Control of 39546-32-2, the publication is ChemistrySelect (2020), 5(45), 14422-14429, database is CAplus.

The present article reported the synthesis of N-(4-(6-chloroH-imidazo[1,2-a]pyridin-2-yl)phenyl)acetamide derivatives (PINRAc) I [R = piperidin-1-yl, morpholin-4-yl, cyclohexylaminyl, etc.] using 5-chloropyridin-2-amine and 2-bromo-1-(4-nitrophenyl)ethanone in a multi-step protocol. The structures of all the compounds I were characterized by NMR, FT-IR and GCMS. The compounds I were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Most of them exhibited good antitubercular activity with MIC in the range of 1.6-25μg/mL and the cytotoxicity study carried out on human embryonic kidney cell line showed no toxicity on the normal cells. The docking study was performed on mycolic acid transporter protein MmpL3 from Mycobacterium smegmatis which supported the in-vitro results.

ChemistrySelect published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Quality Control of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Xing, Hongjie published the artcileUltrasound-assisted synthesized BiFeO₃ as FeOH⁺ promoted peroxymonosulfate activator for highly efficient degradation of tetracycline, Application In Synthesis of 826-36-8, the publication is Journal of Alloys and Compounds (2021), 157281, database is CAplus.

A multiferroic BiFeO3 (BFO) catalyst was fabricated through a mild one-pot hydrothermal process with a bath-ultrasound assisted dissolution of Fe(NO3)3·9H2O for 30 min. X-ray photoemission spectroscopy revealed that the BFO (BFO-u) catalyst with US assisted dissolution of Fe(NO3)3·9H2O in the synthetic process exhibited high Fe2+ and OH- levels, which could be explained to be Fe3+ + H2O → Fe2+ + H+ + •OH. As a result, BFO-u catalyst activated potassium peroxymonosulfate (PMS) efficiently for degrading tetracycline hydrochloride. In particular, visible-light assisted activation of PMS over BFO-u catalyst exhibited the highest degradation rate constant, at 0.352 min-1. Species-trapping experiments revealed that the presence of PMS promoted the generation of •OH, •O-2 and 1O2 that all participated in degrading TCH, in which 1O2 was primarily contributed to the degradation Also, BFO-u catalyst was stable and recyclable and thus suitable for practical applications.

Journal of Alloys and Compounds published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Rzasa, Robert M. published the artcileSynthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility, Safety of Piperidine-4-carboxamide, the publication is Bioorganic & Medicinal Chemistry (2014), 22(23), 6570-6585, database is CAplus and MEDLINE.

We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors. Structure-activity studies improved the solubility (pH 7.4) and maintained high PDE10A activity compared to initial lead compound 3, with select compounds demonstrating good oral bioavailability. X-ray crystallog. studies revealed two distinct binding modes to the catalytic site of the PDE10A enzyme. An ex vivo receptor occupancy assay in rats demonstrated that this series of compounds covered the target within the striatum.

Bioorganic & Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Safety of Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem