Month: November 2022

Takai, Haruki published the artcileSynthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents, COA of Formula: C12H20Cl2N2, the main research area is quinazolinepiperidine derivative preparation antihypertensive; piperidine quinazoline derivative preparation antihypertensive.

A series of piperidine derivatives with a 2-oxo-1,2,3,4-tetrahydro-quinazoline or 2,4-dioxo-1,2,3,4-tetrahydroquinazoline ring at the 4-position were prepared and tested for antihypertensive activity in rats. Among the compds tested, I  [92311-03-0] and II  [92311-10-9] produced relatively strong hypotension in the spontaneously hypertensive rat model.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, COA of Formula: C12H20Cl2N2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rabal, Obdulia published the artcileDiscovery of in Vivo Chemical Probes for Treating Alzheimer’s Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is sildenafil vardenafil orthoaminoanilide synthesis antiAlzheimer SAR PDE5 histone deacetylase; Alzheimer’s disease; PDE5 inhibition; chemical probes; class I HDAC selective inhibition; dual inhibitors; in vivo test.

In order to determine the contributions of histone deacetylase (HDAC) isoforms to the beneficial effects of dual phosphodiesterase 5 (PDE5) and pan-HDAC inhibitors on in vivo models of Alzheimer’s disease (AD), we have designed, synthesized, and tested novel chem. probes with the desired target compound profile of PDE5 and class I HDAC selective inhibitors. Compared to previous hydroxamate-based series, these mols. exhibit longer residence times on HDACs. In this scenario, shorter or longer preincubation times may have a significant impact on the IC50 values of these compounds and therefore on their corresponding selectivity profiles on the different HDAC isoforms. On the other hand, different chem. series have been explored and, as expected, some pairwise comparisons show a clear impact of the scaffold on biol. responses. The lead identification process led to compound I, which shows an adequate ADME-Tox profile and in vivo target engagement (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation) in the central nervous system (CNS), suggesting that this compound represents an optimized chem. probe; thus, I has been assayed in a mouse model of AD (Tg2576).

ACS Chemical Neuroscience published new progress about Alzheimer disease. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zang, Yingda published the artcileClaulansine F-donepezil hybrids as anti-Alzheimer’s disease agents with cholinergic, free-radical scavenging, and neuroprotective activities, Product Details of C10H20N2O2, the main research area is Claulansine donepezil hybrid preparation docking anticholinesterase Alzheimer neuroprotective; AChE inhibitory activity; Alzheimer’s disease; Claulansine F–donepezil hybrids; free-radical scavenging activity; neuroprotective effects.

The multifactorial nature of Alzheimer’s disease (AD) calls for the development of multitarget agents addressing key pathogenic processes. Twenty-six Claulansine F-donepezil hybrids I (X = nothing, CH2, CH2CH2; R1 = OMe, t-Bu; R2 = PhCH2, 2-FC6H4CH2, 4-ClC6H4CH2, etc.) were designed and synthesized as multitarget drugs. Among these compounds, six compounds exhibited excellent acetylcholinesterase (AChE) inhibitory activity (half maximal inhibitory concentration (IC50) 1.63-4.62μM). Moreover, the compound I [X = CH2; R1 = t-Bu; R2 = 2-ClC6H4CH2; (II)] exhibited better neuroprotective effects against OGD/R (oxygen-glucose deprivation/reoxygenation) than lead compound Claulansine F. Furthermore, the compound II could cross the blood-brain barrier in vitro. More importantly, compared to edaravone, the compound II had stronger free-radical scavenging activity. Mol. docking studies revealed that II could interact with the catalytic active site of AChE. All of these outstanding in vitro results indicate the compound II as a leading structure worthy of further investigation.

Molecules published new progress about Alzheimer disease. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Product Details of C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Anderson, Fiona M. published the artcileSynthesis of new homochiral bispyrrolidines as potential DNA cross-linking antitumor agents, COA of Formula: C7H15Cl2N, the main research area is structure activity antitumor bispyrrolidine DNA crosslinking.

We are seeking to develop more effective bifunctional alkylating agents as antitumor agents. We previously synthesized conformationally restricted nitrogen mustards containing one piperidine ring, then bispiperidine derivatives were designed and prepared with varying lengths of carbon chain between the two rings and structure-activity relationships in these systems were studied. A bispiperidine with the shortest bridge of two carbon atoms was the most reactive bifunctional alkylating agent. In order to extend this work and investigate the effects of a change in the size of the heterocyclic systems, new bispyrrolidine salts 17-23 with chloromethyl groups at the 2-positions and a bridge between the two nitrogen atoms of 2-8 carbon atoms were synthesized from L-proline so that only the LL-enantiomers were produced. The free bases were designed to be bifunctional alkylating agents via aziridinium ion formation with different distances between the two alkylating sites. All of the bispyrrolidines were efficient cross-linkers of naked DNA apart from those with three-carbon (18) and four-carbon (19) bridges, in contrast to the results with the bispiperidines. A piperazine derivative 24 with two potential alkylating sites was also shown to be an efficient cross-linker, as was an alicyclic compound 25 with six carbon atoms between the two alkylating sites. Compounds 26 and 30 with an extra carbon atom between the nitrogen and the leaving group were not cross-linkers, as expected if aziridinium ion formation is crucial for crosslinking ability. The preformed aziridine 27 with a further alkylating site was an efficient cross-linker. Compounds 28-29 with only one potential alkylating center were not cross-linkers of DNA. None of the compounds, however, produced significant cytotoxicity in human tumor cells in vitro.

Anti-Cancer Drug Design published new progress about Alkylating agents. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, COA of Formula: C7H15Cl2N.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Guo, Cuiping published the artcileMinimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening, Computed Properties of 73874-95-0, the main research area is proteome profiling cell imaging drug screening linker fluorescent probe.

Activity-based protein profiling (ABPP) and bioimaging have been powerful approaches for in situ drug screening and target identification. However, these approaches are still hindered by the preparation of high-quality probes. To address this challenge, we developed a series of novel minimalist linkers for irreversible inhibitors by incorporation of various bioorthogonal handles into an α,β-unsaturated amide, a common moiety of many irreversible inhibitors. The linker-containing probes have been demonstrated to be suitable for simultaneous protein labeling, live cell imaging and drug screening.

Chemical Communications (Cambridge, United Kingdom) published new progress about Affinity labeling. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Computed Properties of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wallner, Gernot M. published the artcileComparison of Crosslinking Kinetics of UV-Transparent Ethylene-Vinyl Acetate Copolymer and Polyolefin Elastomer Encapsulants, Formula: C28H52N2O4, the main research area is transparent ethylene vinyl acetate copolymer polyolefin elastomer encapsulant crosslinking; EVA; POE; activation energy; crosslinking kinetics; dynamic mechanical analysis; photovoltaics.

Encapsulants based on ethylene-vinyl acetate copolymers (EVA) or polyolefin elastomers (POE) are essential for glass or photovoltaic module laminates. To improve their multi-functional property profile and their durability, the encapsulants are frequently peroxide crosslinked. The crosslinking kinetics are affected by the macromol. structure and the formulation with stabilizers such as phenolic antioxidants, hindered amine light stabilizers or aromatic UV absorbers. The main objective of this study was to implement temperature-rise and isothermal dynamic mech. anal. (DMA) approaches in torsional mode and to assess and compare the crosslinking kinetics of novel UV-transparent encapsulants based on EVA and POE. The gelation time was evaluated from the crossover of the storage and loss shear modulus. While the investigated EVA and POE encapsulants revealed quite similar activation energy values of 155 kJ/mol, the storage modulus and complex viscosity in the rubbery state were significantly higher for EVA. Moreover, the gelation of the polar EVA grade was about four times faster than for the less polar POE encapsulant. Accordingly, the curing reaction of POE was retarded up to a factor of 1.6 to achieve a progress of crosslinking of 95%. Hence, distinct differences in the crosslinking kinetics of the UV-transparent EVA and POE grades were ascertained, which is highly relevant for the lamination of modules.

Polymers (Basel, Switzerland) published new progress about Activation energy. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Formula: C28H52N2O4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Li, Yuchun published the artcileThe synergistic effect between bis(2,2,6,6-tetramethyl-4-piperidyl) sebacate and polysiloxane on the photo-aging resistance and flame retardancy of polypropylene, Computed Properties of 52829-07-9, the main research area is polysiloxane photoaging resistance flame retardancy polypropylene.

The introduction of flame retardants often decreases the UV resistance ability of the photo stabilizer. In this work, the antagonistic effect between APP and a light stabilizer HLAS770 was investigated, and the microencapsulated APP (Si-APP) was prepared by coating ammonium polyphosphate (APP) with polysiloxane. Si-APP was introduced into polypropylene (PP) in association with a light stabilizer bis (2,2,6,6-tetramethyl-4-piperidyl) sebacate (HALS770) to synchronously improve both the photo-aging resistance and flame retardancy. The characterization of surface topog., carbonyl index, and mech. properties demonstrated that the antagonistic effect between APP and HALS770 was eliminated by the presence of polysiloxane. The limiting oxygen index and cone calorimeter test results revealed that the heat and smoke release of aged PP composites containing Si-APP and HALS770 was decreased by 28% and 35% resp., compared with that of the aged control PP sample, which is crucial to the practical application of PP. It was proved that polysiloxane and HALS770 synergistically improved the photo-aging resistance and flame retardancy of PP. It is suggested that this work provides a new strategy for fabricating long-life flame retardant polypropylene composites.

Composites, Part B: Engineering published new progress about Activation energy. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Computed Properties of 52829-07-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kumar, C. B. Pradeep published the artcileFluorine substituted thiomethyl pyrimidine derivatives as efficient inhibitors for mild steel corrosion in hydrochloric acid solution: Thermodynamic, electrochemical and DFT studies, COA of Formula: C10H20N2O2, the main research area is fluorine substituted thiomethyl pyrimidine derivative steel corrosion inhibitor thermodn.

Three new 5-fluoro-2- methylthio substituted pyrimidine derivatives have been synthesized and characterized by 1H NMR spectroscopy and Mass spectrometry. Corrosion inhibition characteristics of the synthesized pyrimidine derivatives have been studied on mild steel (MS) in 0.5 M hydrochloric acid solution at various temperatures (303-333 K) using mass loss and electrochem. techniques. The obtained weight loss, electrochem. impedance and potentiodynamic polarization data indicate that the corrosion inhibition efficiency is directly proportional to concentration of the inhibitors. The Adsorption process on MS surface obeyed Langmuir isotherm model. SEM (SEM) was used to characterize surface morphol. of the MS specimen in absence and presence of pyrimidine derivatives D. functional theory (DFT) calculations using B3LYP functional with 6-311+G (d,p) level was used to establish the relationship between mol. structure and corrosion inhibition efficiency. Electrochem. anal. indicated that pyrimidine derivatives inhibit the corrosion by adsorbing on the metal surface. Mixed-type of corrosion inhibition activity with anodic predominance was proposed by polarization studies.

Journal of Molecular Liquids published new progress about Activation energy. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, COA of Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Hu, Guodong published the artcileDepletion of protein thiols and the accumulation of oxidized thioredoxin in Parkinsonism disclosed by a red-emitting and environment-sensitive probe, Application In Synthesis of 73874-95-0, the main research area is fluorescent probe imaging protein thiol oxidized thioredoxin Parkinsonism model.

Protein sulfhydryl groups play a vital role in maintaining cellular redox homeostasis and protein functions and have attracted increasing interests for the selective detection of protein thiols over low-mol.-weight thiols (LMWTs). Herein, we reported a red-emitting and environment-sensitive probe (FM-red) for detecting and labeling protein thiols. The probe contains a maleimide unit as a thiol receptor and an environment-sensitive fluorophore as a sensor. The emission signal of the probe was exclusively switched on by binding to protein sulfhydryl groups through the twisted intramol. charge transfer mechanism, while negligible fluorescence was observed when FM-red reacted with LMWTs. Various experiments verified that FM-red possessed fast responsivity (∼10 min) and high selectivity to sense protein thiols over LMWTs with a red emission (∼655 nm). These favorable properties enable the probe to image protein sulfhydryl groups in live cells and in vivo. In addition, as FM-red has a relatively high mol. weight (MW 688), it is able to sep. the labeled proteins from the unlabeled ones after FM-red derivatization via routine protein electrophoresis, which may be applied to determine the redox states of thioredoxin, a small redox protein ubiquitous in all cells. With the aid of the probe, we demonstrated a significant decrease in the protein thiols and the accumulation of oxidized thioredoxin in a cellular model of Parkinson’s disease.

Journal of Materials Chemistry B: Materials for Biology and Medicine published new progress about Biological imaging. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Srirodpai, Onruthai published the artcilePreparation, characterizations and oxidation stability of polyethylene coated nanocrystalline VO2 particles and the thermo-chromic performance of EVA/VO2@PE composite film, Quality Control of 52829-07-9, the main research area is ethylene vinyl acetate copolymer vanadium dioxide polyethylene film.

In this study, an alternative approach is presented for developing thermo-chromic film, based on ethylene vinyl acetate copolymer (EVA) and vanadium dioxide (VO2) composite, with enhanced oxidation stability and compatibility. The neat monoclinic nanocrystalline VO2 particles were firstly prepared via a hydrothermal process, using citric acid as a reducing agent. After that, the synthesized VO2 particles were characterized, prior to mixing with maleic anhydride grafted PE. The crystalline structure, morphol. and thermochromic performance of the polyethylene coated vanadium dioxide (VO2@PE) particles were then verified by SEM, TEM, DSC, XRD, FTIR techniques. After coating, a better oxidation stability of the VO2 particles was noted while the thermo-chromic performance of the VO2@PE was also maintained. After mixing with EVA, the percentage strain and tensile toughness of the VO2@PE based EVA films was the highest, followed by those of the uncoated VO2-based EVA films and the neat EVA, resp. The VO2@PE-based films also maintained the thermochromic behavior of the monoclinic VO2. The above improvements were achieved at the expense of percentages of visible light transmittance and gel content of the EVA. This is the first report of the EVA/VO2-based thermo-chromic film, which is tougher and more stable toward oxidation than the prior state of the art. This composite film has the potential to be used as a kind of a specialty lamination material for smart windows and energy efficiency in buildings.

Journal of Nanoscience and Nanotechnology published new progress about Elongation at break. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Quality Control of 52829-07-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem