Month: November 2022

Falsini, Matteo published the artcileNew 8-amino-1,2,4-triazolo[4,3-a]pyrazin -3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A_2A adenosine receptor antagonists, Product Details of C6H12N2O, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(11), 127126, database is CAplus and MEDLINE.

In this work, further structural investigations on the 8-amino-2-phenyl-6-aryl-1,2,4-triazolo[4,3-a]pyrazin-3-one series were carried out to achieve potent and selective human A_2A adenosine receptor (AR) antagonists. Different ether and amide moieties were attached at the para-position of the 6-Ph ring, thus leading to compounds 1-9 and 10-18, resp. Most of these moieties contained terminal basic rings (pyrrolidine, morpholine, piperidine and substituted piperazines) which were thought to confer good physicochem. and drug-like properties. Compounds 11-16, bearing the amide linker, possessed high affinity and selectivity for the hA_2A AR (K_i = 3.6-11.8 nM). Also derivatives 1-9, featuring an ether linker, preferentially targeted the hA_2A AR but with lower affinity, compared to those of the relative amide compounds Docking studies, carried out at the hA_2A AR binding site, highlighted some crucial ligand-receptor interactions, particularly those provided by the appended substituent whose nature deeply affected hA_2A AR affinity.

Bioorganic & Medicinal Chemistry Letters 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, Product Details of C6H12N2O.

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

Loman, Jacob. J. published the artcileA combined computational and experimental investigation of the oxidative ring-opening of cyclic ethers by oxoammonium cations, Recommanded Product: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, the publication is Organic & Biomolecular Chemistry (2016), 14(16), 3883-3888, database is CAplus and MEDLINE.

The propensity of oxoammonium cations to facilitate the oxidative ring-opening of cyclic ethers to their corresponding distal hydroxy ketones is investigated. The reaction has been evaluated using exptl. and computational methods to gain deeper insight into trends in reactivity.

Organic & Biomolecular Chemistry published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Recommanded Product: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate.

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

Winterton, Sarah E. published the artcileDiscovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase, COA of Formula: C20H22ClN3O3, the publication is Journal of Medicinal Chemistry (2018), 61(12), 5199-5221, database is CAplus and MEDLINE.

Stearoyl-CoA desaturase (SCD) catalyzes the first step in the conversion of saturated fatty acids to unsaturated fatty acids. Unsaturated fatty acids are required for membrane integrity and for cell proliferation. For these reasons, inhibitors of SCD represent potential treatments for cancer. However, systemically active SCD inhibitors result in skin toxicity, which presents an obstacle to their development. We recently described a series of oxalic acid diamides that are converted into active SCD inhibitors within a subset of cancers by CYP4F11-mediated metabolism Herein, we describe the optimization of the oxalic acid diamides and related N-acyl ureas and an anal. of the structure-activity relationships related to metabolic activation and SCD inhibition.

Journal of Medicinal Chemistry 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 C13H19BN2O3, COA of Formula: C20H22ClN3O3.

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

Li, Guang published the artcileFe₃O₄ supported on water caltrop-derived biochar toward peroxymonosulfate activation for urea degradation: the key role of sulfate radical, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2022), 433(Part_2), 133595, database is CAplus.

A new type of iron-doped and porous biochar (Fe@BC) derived from water caltrop was systematically investigated to catalyze the organic pollutants degradation by peroxymonosulfate (PMS). The effectiveness of this novel material was tested by treating excessive urea concentrations in swimming pool water. It exhibited good PMS activation capacity, achieving urea removal of 100% within 15 min. The Fe@BC/PMS system exhibited excellent resistance to common anions. Only chloride showed a small inhibitory effect, and the removal efficiency of urea decreased by 10% ([Cl^–]₀ = 10 mM). Quenching experiments and ESR spectroscopy analyses demonstrated that urea degradation was mainly mediated by the radical pathway, which in turn was dominated by surface-bound sulfate radicals (SO₄^·-). Further, reusability experiments confirmed the stability of the material. After three cycles, the degradation efficiency can still reach 86%. Therefore, the conversion of water caltrop-derived biochar into a composite catalytic material provides a novel strategy for value-added utilization of aquatic waste biomass, and it is also a promising alternative for the treatment of urea from swimming pool water.

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 C9H17NO, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one.

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

Liang, Huazhe published the artcilePolyamidoamine Immobilized TEMPO Mediated Oxidation of Cellulose: Effect of Macromolecular Catalyst Structure on the Reaction Rate, Oxidation Degree and Degradation Degree, Application In Synthesis of 826-36-8, the publication is Fibers and Polymers (2020), 21(6), 1251-1258, database is CAplus.

A series of polyamidoamine (PAMAM) immobilized TEMPO macromol. catalysts were prepared by condensation reduction reactions between carbonyl groups in 4-O-TEMPO and primary amines in PAMAM. The macromol. catalyst and NaBr/NaClO were used as catalytic system for selective oxidation of cellulose in aqueous medium. Effects of various factors, such as TEMPO loading ratios and PAMAM generations, were studied on the catalytic performances. Compared with free TEMPO, the macromol. catalyst with less than 50% TEMPO loading ratio had a higher reaction rate in the initial stage of the reaction. Especially, the reaction rate of G1.0 PAMAM with 30% TEMPO loading ratio was comparable to free TEMPO in the whole reaction process. Its cellulose oxidation degree (or catalytic activity) was also equivalent to the level of free TEMPO. Interestingly, the cellulose depolymerization degree of macromol. catalyst was not affected by the cellulose oxidation degree and was lower than that of free TEMPO. The macromol. catalyst could be recycled efficiently by the combination of supernatant circulation and salting-out extraction, and the recycling performance was excellent.

Fibers and Polymers 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, Application In Synthesis of 826-36-8.

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

Gandioso, Albert published the artcileA Green Light-Triggerable RGD Peptide for Photocontrolled Targeted Drug Delivery: Synthesis and Photolysis Studies, Product Details of C19H21N, the publication is Journal of Organic Chemistry (2016), 81(23), 11556-11564, database is CAplus and MEDLINE.

We describe for the first time the synthesis and photochem. properties of a coumarin-caged cyclic RGD peptide and demonstrate that uncaging can be efficiently performed with biol. compatible green light. This was accomplished by using a new dicyanocoumarin derivative (DEAdcCE) for the protection of the carboxyl function at the side chain of the aspartic acid residue, which was selected on the basis of Fmoc-tBu SPPS compatibility and photolysis efficiency. The shielding effect of a Me group incorporated in the coumarin derivative near the ester bond linking both moieties in combination with the use of acidic additives such as HOBt or Oxyma during the basic Fmoc-removal treatment were found to be very effective for minimizing aspartimide-related side reactions. In addition, a conjugate between the dicyanocoumarin-caged cyclic RGD peptide and ruthenocene, which was selected as a metallodrug model cargo, has been synthesized and characterized. The fact that green-light triggered photoactivation can be efficiently performed both with the caged peptide and with its ruthenocenoyl bioconjugate reveals great potential for DEAdcCE-caged peptide sequences as selective drug carriers in the context of photocontrolled targeted anticancer strategies.

Journal of Organic Chemistry 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, Product Details of C19H21N.

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

Sheppard, Daniel J. published the artcileComparison of disaccharide donors for heparan sulfate synthesis: uronic acids vs. their pyranose equivalents, HPLC of Formula: 4972-31-0, the publication is Organic & Biomolecular Chemistry (2020), 18(25), 4728-4733, database is CAplus and MEDLINE.

Late oxidation of hexose based building blocks or the use of uronic acid containing building blocks are two complementary strategies in the synthesis of glycosaminoglycans. Here we report the synthesis and evaluation of various disaccharide donors-uronic acids and their pyranose equivalent-for the synthesis of heparan sulfate, using an established protective group strategy. Hexose based “imidate” type donors perform well in the studied glycosylation, while their corresponding uronate esters fall short; a uronate ester thioglycoside performs equal to, if not better than, a hexose thioglycoside equivalent

Organic & Biomolecular 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 C4H4N2O2, HPLC of Formula: 4972-31-0.

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

Ribeiro da Silva, Manuel A. V. published the artcileExperimental Study on the Thermochemistry of Some Derivatives of Piperidinol, Application of 1-Ethylpiperidin-3-ol, the publication is Journal of Chemical & Engineering Data (2006), 51(2), 767-771, database is CAplus.

Standard (p° = 0.1 MPa) energies of combustion for 1-methyl-3-piperidinol, 1-ethyl-3-piperidinol, and 1-methyl-4-piperidinol were measured at 298.15 K by static bomb calorimetry. The standard molar enthalpies of formation of the condensed phase were derived. The standard molar enthalpies of vaporization at 298.15 K of the three piperidinol derivatives studied were determined by high-temperature Calvet microcalorimetry. The resp. standard molar enthalpies of formation in the gaseous phase at 298.15 K were derived.

Journal of Chemical & Engineering Data 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 C7H15NO, Application of 1-Ethylpiperidin-3-ol.

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

Hong, Misun published the artcileSinglet Oxygen in Lithium-Oxygen Batteries, Related Products of piperidines, the publication is Batteries & Supercaps (2021), 4(2), 286-293, database is CAplus.

A review. Singlet oxygen (¹O₂) is one of the most critical species leading to parasitic side reactions and poor reversibility in non-aqueous Li-O₂ batteries. ¹O₂ is generated via the disproportionation of the superoxide radical (O₂.-) in O₂/Li₂O₂ electrochem. The mechanistic and computational studies on ¹O₂ formation revealed the significant roles of the associated cations, solvation ability of aprotic solvents, H⁺ source, and catalyst/electrode materials. Along with efforts to alleviate ¹O₂ production, trapping and eliminating ¹O₂ have been attempted using mol. agents. Anthracene derivatives trap ¹O₂ and form endoperoxides, which can be quant. detected using in situ fluorescence anal. Phys. quenchers that convert ¹O₂ to ³O₂ are desirable for cycling of Li-O₂ cells because quencher mols. are reusable. We highlight the recent reports on the formation and elimination of ¹O₂, and challenges and perspectives of suppressing the ¹O₂ effect on the performance of Li-O₂ cells.

Batteries & Supercaps 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, Related Products of piperidines.

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

Kosak, Urban published the artcileStraightforward synthesis of orthogonally protected piperidin-3-ylmethanamine and piperidin-4-ylmethanamine derivatives, Related Products of piperidines, the publication is Tetrahedron Letters (2014), 55(12), 2037-2039, database is CAplus.

The synthesis of orthogonally protected piperidin-3-ylmethanamines and piperidin-4-ylmethanamines from com. available nipecotamide, isonipecotamide, nipecotic acid, and isonipecotic acid was presented. This is a straightforward 2-step procedure that gives high overall yields. Purification of the intermediates is not necessary, and the final compounds are purified by simple flash column chromatog.

Tetrahedron Letters 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, Related Products of piperidines.

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