Month: November 2022

Li, Zhuoqian published the artcileActivation of peroxymonosulfate by iron-biochar composites: Comparison of nanoscale Fe with single-atom Fe, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Journal of Colloid and Interface Science (2021), 582(Part_B), 598-609, database is CAplus and MEDLINE.

A convenient and efficient method to fabricate isolated Fe single-atom catalysts deposited on Myriophyllum aquaticum-based biochar (ISA-Fe/MC) is reported for peroxymonosulfate-based organics degradation Firstly, the Fe nanoparticles anchored on the hierarchical porous biochar (nano-Fe/MC) can be obtained by utilizing K₂FeO₄ as a synchronous activation and graphitization agent. Subsequently, ISA-Fe/MC was achieved by HCl etching of nano-Fe/MC to remove the excess Fe nanoparticles. Compared with nano-Fe/MC, ISA-Fe/MC demonstrated outperformed catalytic capacity towards PMS activation for phenol degradation The combination of super high surface area, hierarchical porous structure, graphitization structure and atomically dispersed Fe species should be responsible for prominent catalytic oxidation ability and outstanding resistance to common anions and humic acid. Based on the chem. scavengers, EPR experiments and electrochem. tests, the SO^â€?₄ dominated radical degradation pathway for nano-Fe/MC and electron transfer reigned non-radical degradation pathway for ISA-Fe/MC was revealed. In contrast to nano-Fe/MC, d. functional theory calculations demonstrated the enhanced d. of states around Fermi level in ISA-Fe/MC meaning the increased catalytic performance and more electron transfer between single-atom Fe to adjacent graphitic C and N which could serve as electron transfer channel for PMS activation.

Journal of Colloid and Interface Science 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 C9H17NO, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one.

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

Crich, David published the artcileSynthesis of the Salmonella Type E₁ Core Trisaccharide as a Probe for the Generality of 1-(Benzenesulfinyl)piperidine/Triflic Anhydride Combination for Glycosidic Bond Formation from Thioglycosides, Name: 1-(Phenylsulfinyl)piperidine, the publication is Journal of Organic Chemistry (2002), 67(14), 4640-4646, database is CAplus and MEDLINE.

A synthesis of a chromogenic glycoside of the Salmonella anatum group E₁ core trisaccharide is presented in which all three glycosidic bonds, a 1,2-cis-equatorial, a 1,2-trans-axial, and a 1,2-trans-equatorial linkage representing three of the four main classes of glycosidic bond, are formed with thioglycoside donors activated under a single set of conditions by the combination of 1-(benzenesulfinyl)piperidine and trifluoromethanesulfonic anhydride. 2,3-O-Carbonyl- and 2,3-O-isopropylidene-α-L-rhamnopyranosyl thioglycosides are found to be highly α-selective rhamnosyl donors under these conditions.

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, Name: 1-(Phenylsulfinyl)piperidine.

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

Ji, Qinggang published the artcileDesign, synthesis and biological evaluation of novel diazaspirodecanone derivatives containing piperidine-4-carboxamide as chitin synthase inhibitors and antifungal agents, Name: Piperidine-4-carboxamide, the publication is Bioorganic Chemistry (2021), 105108, database is CAplus and MEDLINE.

A series of novel 2-oxo-(1-oxo-2,8-diazaspiro[4.5]decane-8-yl)ethylpiperidine carboxamide derivatives were designed, synthesized and characterized by 1H NMR, 13C NMR and HRMS spectroscopy. All eighteen newly prepared compounds were evaluated for their inhibition against chitin synthase (CHS) and antifungal activities in vitro. The enzyme assay revealed that compound 5h showed excellent inhibitory activity against CHS with IC50 value of 0.10 mM, and the compounds 5b, 5d and 5q showed good inhibition against chitin synthase with IC50 values of 0.13 mM, 0.18 mM and 0.15 mM, resp., while IC50 value of ployoxin B was 0.08 mM. Meanwhile, the others of these compounds exhibited moderate inhibition potency against chitin synthase. The antifungal assay showed compound 5h had excellent antifungal activity compared with the control drugs fluconazole and polyoxin B against these tested strains including C. albicans, A. fumigatus, C. neoformans and A. flavus. Its excellent antifungal activity was consistent with its excellent chitin synthase inhibition. Compound 5k and 5l against C. albicans were comparable with fluconazole, and they showed strong antifungal potency against A. flavus with MIC values of 0.07 mmol/L and 0.13 mmol/L resp. Compound 5m had similar MIC value against A. fumigatus to fluconazole. The phenomenon that compounds 5b, 5d and 5q that showed good enzymic inhibition didnt exert good antifungal activity, while compounds 5k, 5l and 5m that showed moderate chitin synthase inhibition exhibited excellent antifungal activity was discussed. Furthermore, the trial of drug combination showed that compounds had synergistic effects or additive effects with fluconazole against tested fungi which also verified that these designed compounds targeted different targets from that of fluconazole. Addnl., the antibacterial trial showed that all synthesized compounds had little potency against tested bacteria strains. These results indicated that the designed compounds were potential chitin synthase inhibitors and had selectively antifungal activities.

Bioorganic 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, Name: Piperidine-4-carboxamide.

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

Sutherland, Mathew published the artcileRational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics, SDS of cas: 2757618-86-1, the publication is ChemMedChem (2021), 16(7), 1116-1125, database is CAplus and MEDLINE.

Protein arginine N-Me transferase 4 (PRMT4) asym. dimethylates the arginine residues of histone H3 and nonhistone proteins. The overexpression of PRMT4 in several cancers had stimulated interest in the discovery of inhibitors as biol. tools and, potentially, therapeutics. Although several PRMT4 inhibitors had reported, most display poor selectivity against other members of the PRMT family of Me transferases. Herein, the structure-based design of a new class of alanine-containing 3-arylindoles such as I [R = Me, i-Pr, NMe₂, etc.] as potent and selective PRMT4 inhibitors was reported, and described key structure-activity relationships for this class of compounds

ChemMedChem published new progress about 2757618-86-1. 2757618-86-1 belongs to piperidines, auxiliary class Boronic acid and ester, name is 1-((3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)piperidine, and the molecular formula is C6H12Br2, SDS of cas: 2757618-86-1.

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

Kuehl, Nikos published the artcileBeyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture, Quality Control of 39546-32-2, the publication is Journal of Medicinal Chemistry (2021), 64(8), 4567-4587, database is CAplus and MEDLINE.

The viral serine protease NS2B-NS3 is one of the promising targets for drug discovery against dengue virus and other flaviviruses. The mol. recognition preferences of the protease favor basic, pos. charged moieties as substrates and inhibitors, which leads to pharmacokinetic liabilities and off-target interactions with host proteases such as thrombin. We here present the results of efforts that were aimed specifically at the discovery and development of noncharged, small-mol. inhibitors of the flaviviral proteases. A key factor in the discovery of these compounds was a cellular reporter gene assay for the dengue protease, the DENV2proHeLa system. Extensive structure-activity relationship explorations resulted in novel benzamide derivatives with submicromolar activities in viral replication assays (EC₅₀ 0.24μM), selectivity against off-target proteases, and negligible cytotoxicity. This structural class has increased drug-likeness compared to most of the previously published active-site-directed flaviviral protease inhibitors and includes promising candidates for further preclin. development.

Journal of 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, Quality Control of 39546-32-2.

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

Van Luppen, J. J. published the artcileNMR study on trapping techniques to deduce the conformations of 1-alkyl-3-hydroxypiperidines, Product Details of C7H15NO, the publication is Organic Magnetic Resonance (1982), 18(4), 199-206, database is CAplus.

The conformational equilibrium of the title compounds [I; R = H, Me, Et, Pr, Bu, CHMe₂, CHMeEt, (CH₂)₄Me, CHMePr] was examined in hexane and H₂O. The most reliable results were obtained by conformational trapping in D₂SO₄/D₂O and anal. by ¹H and ¹³C NMR. In an apolar solvent, the conformation with an axial group always predominates (69%). In aqueous acid solution of pH 5 the same conformation predominates (56%); in aqueous base of pH âˆ?1 the axial-OH conformer accounted for only 43% of the mols. The results were compared with those obtained by other methods, e.g. IR.

Organic Magnetic Resonance published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C19H17N2NaO4S, Product Details of C7H15NO.

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

Sun, Xiaoqing published the artcileLong-Lasting and Intense Chemiluminescence of Luminol Triggered by Oxidized g-C₃N₄ Nanosheets, Name: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Analytical Chemistry (Washington, DC, United States) (2020), 92(17), 11860-11868, database is CAplus and MEDLINE.

Most of the known chemiluminescence (CL) systems are flash-type, whereas a CL system with long-lasting and strong emission is very favorable for accurate CL quant. anal. and imaging assays. In this work, we found that the oxidized g-C₃N₄ (g-CN_OX) could trigger luminol-H₂O₂ to produce a long-lasting and intense CL emission. The CL emission lasted for over 10 min and could be observed by the naked eye in a dark room. By means of a CL spectrum, X-ray photoelectron spectra, and ESR spectra, the possible mechanism of this CL reaction was proposed. This strong and long-duration CL emission was attributed to the high catalytic activity of g-CN_OX nanosheets and continuous generation of reactive oxygen species from H₂O₂ on g-CN_OX surface. Taking full advantage of the long-lasting CL property of this system, we proposed one “non-in-situ mixing” mode of CL measurement. Compared with the traditional “in-situ mixing” CL measurement mode, this measurement mode was convenient to operate and had good reproducibility. This work not only provides a long-lasting CL reaction but also deepens the understanding of the structure and properties of g-C₃N₄ material.

Analytical Chemistry (Washington, DC, United States) 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 C9H11NO4, Name: 2,2,6,6-Tetramethylpiperidin-4-one.

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

Morelli, Laura published the artcile2,3-Carbamate mannosamine glycosyl donors in glycosylation reactions of diacetone-D-glucose. An experimental and theoretical study, Computed Properties of 4972-31-0, the publication is Carbohydrate Research (2021), 108421, database is CAplus and MEDLINE.

The role of the cyclic 2,3-N,O-carbamate protecting group in directing the selectivity of mannosylation reactions of diacetone-D-glucose, promoted by BSP/Tf₂O via α-triflate intermediates, has been investigated through a combined computational and exptl. approach. DFT calculations were used to locate the transition states leading to the α or β anomers. These data indicate the preferential formation of the β-adduct with mannosyl donors either equipped with the 4,6-O-benzylidene protection or without it. The synthetic results confirmed this preference, showing in both cases an α/β selectivity of 4:6. This highlights a role for the 2,3-N,O-carbamate in sharp contrast with what described in the case of 2,3-O-carbonate mannosyl donors.

Carbohydrate Research 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, Computed Properties of 4972-31-0.

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

Wudl, Fred published the artcileAsymmetric synthesis of chiral sulfoxides. II. Intramolecular oxygen to nitrogen sulfinyl migration, Synthetic Route of 4972-31-0, the publication is Journal of the American Chemical Society (1973), 95(19), 6349-58, database is CAplus.

The conversion of a 1,2,3-oxathiazolidine 2-oxide (I), derived from l-ephedrine, to Me aryl sulfoxides via sulfinamides (II; R = Me, Ph, MeC6H4) was studied in detail. The stereochem. of sulfinyl transfer in an O-sulfinylated ethanolamine (III) was investigated. This rearrangement proceeds via two competitive paths: intramol. and intermol. The intramol. path yields II with retention of configuration at S.

Journal of the American Chemical Society 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 C7H8O3, Synthetic Route of 4972-31-0.

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

Kim, Eunha published the artcileInhibition of stearoyl-CoA desaturase1 activates AMPK and exhibits beneficial lipid metabolic effects in vitro, Recommanded Product: 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, the publication is European Journal of Pharmacology (2011), 672(1-3), 38-44, database is CAplus and MEDLINE.

Stearoyl-CoA desaturase1 (SCD1) whole body deficiency protects mice from diet-induced obesity. However the specific mechanism of how SCD1 deficiency protects mice from obesity is not clear yet. To understand the tissue-specific role of SCD1 in energy homeostasis, we investigated the responses of adipocytes, hepatocytes and myotubes to SCD1 inhibition. 3T3-L1 adipocytes treated with a SCD1 inhibitor had decreased expression of lipogenic genes including fatty acid synthase (FAS), acetyl-CoA carboxylase (ACC), and sterol-regulatory element binding protein 1c (SREBP1c) while the expression of fatty acid oxidative genes including carnitine palmitoyltransferase 1 (CPT1), uncoupling protein 2 (UCP2), and peroxisome proliferator-activated receptor gamma coactivator 1-α (PGC1-α) remained unaltered. In mouse primary hepatocytes, treatment with the inhibitor reduced the expression of FAS, ACC, and SREBP1c but increased the expression of fatty acid oxidative genes including acyl-CoA oxidase (AOX), CPT1, and PGC1-α. In addition, inhibitor-treated C2C12 myotubes showed decrease in ACC and FAS expression and increase in expression of CPT1, AOX and PGC1-α. AMP-activated protein kinase (AMPK) is known to regulate cellular metabolism in response to available energy and AMPK activation is associated with enhancement of fatty acid oxidation and suppression of lipogenesis. In all tested cell models, AMPK phosphorylation was increased significantly when SCD1 was inhibited. Taken together, our results indicate that inhibition of SCD1 activity has beneficial lipid metabolic effects of decreased lipogenesis and/or increased fatty acid oxidation, which is at least in part due to an increase of AMPK activation.

European Journal of Pharmacology published new progress about 1032229-33-6. 1032229-33-6 belongs to piperidines, auxiliary class Metabolic Enzyme,SCD, name is 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, and the molecular formula is C20H22ClN3O3, Recommanded Product: 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide.

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