Category: piperidines

Ye, Wenjun published the artcileDesign, synthesis and biological evaluation of novel triazoloquinazolinone and imidazoquinazolinone derivatives as allosteric inhibitors of SHP2 phosphatase, Product Details of C10H20N2O2, the main research area is melanoma SHP2 phosphatase triazoloquinazolinone imidazoquinazolinone; SHP2; allosteric inhibitors; antitumor activity; synthesis.

A series of novel triazoloquinolinone and imidazoquinazolinone derivatives were designed and synthesized, and their biol. activities against SHP2 protein and melanoma A357 cell line were evaluated in vitro. The results show that some target compounds have moderate to excellent inhibitory activity on SHP2 protein and melanoma A357 cell line. Structure-activity relationships (SARs) showed that both imidazoquinazolinone and triazoloquinazolinone derivatives have good SHP2 protein kinase and melanoma cell line A357 inhibitory activity. The results of mol. docking also showed that the cores of imidazoquinazolinone and triazoloquinazolinone have a certain affinity for SHP2 protein at the same time. Compared with SHP244, the target compounds have quite good liver microsomal stability and has more drug potential. The most promising compound has a strong inhibitory effect on the melanoma cell line A357 at 100 μM (76.15% inhibition).

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Melanoma. 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

Peindy N’Dongo, Harmel W. published the artcilePreparation and biological evaluation of cyclopentadienyl-based 99mTc-complexes [(Cp-R)99mTc(CO)3] mimicking benzamides for malignant melanoma targeting, Quality Control of 1205-72-7, the main research area is cyclopentadienyl technetium 99m complex preparation melanoma imaging.

The biol. evaluation of half-sandwich 99mTc-complexes that surrogate iodobenzamide with a high affinity for melanin tumor tissue is described. We have synthesized via retro Diels-Alder reaction two models of 99mTc complexes which possess the piano stool [Cp99mTc(CO)3] motif instead of a Ph ring as in the original iodobenzamide 123I-N-(N-benzylpiperidin-4-yl)-2-iodobenzamide (2-IBP) and N-(2-diethylaminoethyl)-4-iodobenzamide (BZA). Diels-Alder products 2a-2b (HCp-CONHR)2 (2a, R=2-diethylaminoethyl; 2b, R=benzylpiperidin-4-yl) were prepared and reacted with fac-[99mTc(H2O)3(CO)3]+ 1 in water to produce the corresponding 99mTc complexes [(2a)99mTc(CO)3] 4a and [(2b)99mTc(CO)3] 4b. The structures of the 99mTc complexes on the no-carrier-added level have been confirmed by chromatog. comparison with the corresponding rhenium complexes and, macroscopically characterized by IR, NMR, ESI-MS and X-ray crystallog. for [triclinic, P-1, a=7.3518(1) Å, b=8.0309(2) Å, c=17.5536(3) Å, α=99.1260(5)°, β=90.4215(14)°, γ=117.0187(11)°]. The radioconjugate showed good in vitro stability. In murine melanoma B16F1 cells, significant cellular uptake (43.9% of the total applied activity) was attained after 4 h at 37°C with about 50% of the cell-associated radioactivity being internalized in the cells (22% of the applied activity). Furthermore, in melanoma-bearing C57BL6 mice, tumor uptake values of 3.39±0.50 %ID g-1 and 3.21±0.26 %ID g-1 at 1 and 4 h postinjection, resp., were observed indicating a good retention of in the tumor.

Nuclear Medicine and Biology published new progress about Melanoma. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Quality Control of 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Xi published the artcileDielectric Properties of Biaxially Oriented Polypropylene Nanocomposites Prepared Based on Reactor Granule Technology, COA of Formula: C28H52N2O4, the main research area is dielec biaxially oriented polypropylene nanocomposite reactor granule technol.

The addition of inorganic nanoparticles is one of the most widely studied strategies to improve dielec. properties of thin film capacitors, but its application to biaxially oriented polypropylene (BOPP) has rarely been reported due to the difficulty of stretching without break. Here, we have investigated dielec. properties of BOPP/TiO2 nanocomposites prepared by a reactor granule technol., in which precursors impregnated in the pores of PP reactor granule are converted into highly dispersed oxide nanoparticles during melt mixing. The permittivity of the nanocomposites was greatly enhanced beyond classical mixing rules by the addition of a small amount of TiO2 nanoparticles (1-5 wt %), and the enhancement was very sensitive to the stretching ratio. A critical role of the interphase region was suggested. The AC breakdown voltage (BDV) of the BOPP/TiO2 nanocomposites decreased sharply with respect to the amount of TiO2 added. The detailed anal. suggested the roughening of the film surface around the nanoparticles due to stretching as the main cause of the BDV reduction

ACS Applied Electronic Materials published new progress about Antioxidants. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, COA of Formula: C28H52N2O4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kot, David published the artcilePorous graphite as stationary phase for the chromatographic separation of polymer additives – determination of adsorption capability by Raman spectroscopy and physisorption, Related Products of piperidines, the main research area is porous graphite stationary phase chromatog separation polymer additive antioxidant; adsorption capability Raman spectroscopy physisorption polyolefin light stabilizer; Adsorption potential distributions; Brunauer emmett teller (BET) method; HPLC of polymer additives; Polyolefins; Porous graphitic carbon; Raman spectroscopy.

Additives are added to polymers in small concentration to achieve desired application properties widely used to tailor the properties. The rapid diversification of their mol. structures, with often only minute differences, necessitates the development of adequate chromatog. techniques. While modified silica so far is the workhorse as stationary phase we have probed the potential of porous graphitic carbon (HypercarbTM) for this purpose. The results show that the multitude of physicochem. interactions between analyte mols. and the graphitic surface enables separations of polyolefin stabilizers with unprecedented selectivity. To support the chromatog. results the adsorption capability of HypercarbTM for selected antioxidants and UV absorbers was determined by Raman spectroscopy and argon physisorption measurements. The shift of the Graphite-band in the Raman spectra of HypercarbTM upon infusion with additives correlates with the changes in the Adsorption Potential Distributions. The results of argon physisorption measurements go hand in hand with the chronol. of desorption of the additives in liquid chromatog. experiments The elution sequence can be explained by van der Waals or London forces, π-π-interactions and electron lone pair donor-acceptor interactions between the graphite surface and analyte functional groups.

Journal of Chromatography A published new progress about Antioxidants. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Related Products of piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Twigg, Christopher published the artcilePeroxide-initiated chemical modification of polyolefins: In search of a latent antioxidant, Formula: C28H52N2O4, the main research area is peroxide initiated polyolefin antioxidant.

The ability of piperidine-based compounds to confer oxidative stability to polyolefin thermosets without compromising the yields of peroxide-initiated crosslinking and monomer grafting is demonstrated. Unlike phenolic, nitroxyl and phosphite antioxidants that lower the concentration of macroradical intermediates that support polyolefin modifications, additives based upon 2,2,6,6-tetramethylpiperidine (TEMPH) are shown to have little to no effect on the extent of LLDPE crosslinking or the conversion of vinyltriethoxysilane (VTEOS) to grafted hydrocarbon adducts. Notwithstanding this lack of interference in radical-mediated polymer modification, this class of hindered light stabilizer (HAS) compounds are shown to limit the extent of radical oxidation of linear low-d. polyethylene (LLDPE) in an accelerated aging test. The origins of this paradox are discussed in terms of the current state of knowledge regarding HAS activation. The latent antioxidant concept is extended to an alternate approach, wherein 4-acryloyloxy-2,2,6,6-tetramethylpiperidine-N-oxyl (AOTEMPO) is used as an alkyl radical scavenger bearing an oligomerizable functional group. When added at a fraction of the peroxide loading used to produce an LLDPE thermoset, ATEMPO is shown to provide a predictable induction delay without impacting ultimate crosslink d., and produces polymer-bound alkoxyamine functionality that stabilizes the product against oxidation

Polymer published new progress about Antioxidants. 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

Gajdosova, Veronika published the artcilePro-oxidant activity of biocompatible catechin stabilizer during photooxidation of polyolefins, HPLC of Formula: 52829-07-9, the main research area is oxidative biocompatible catechin stabilizer photooxidation polyolefin.

Polymer plaques made of high-d. polyethylene (HDPE) or cycloolefin copolymer (COC) were stabilized with natural phenolic stabilizer (+)-catechin (CAT) and aged using accelerated weathering technique (WOM; accelerated photooxidation). The efficiency of the phenolic stabilizer was compared with a well-established hindered amine stabilizer (HAS) Tinuvin770 (Tin770). In pursuit of the stabilization and identification of short-living radicals generated in the process of photooxidation of the polymers, a spin trapping agent 2,4,6-tri-tert-butylnitrosobenzene (TTBNB) was added to selected samples. Profiles of oxidation products and crystallinity inside the HDPE plaques were determined by IR microspectroscopy, oxidation products in COC copolymers were identified using ATR spectroscopy, concentration profiles of radicals generated inside polymer plaques during WOM exposure were determined by ESRI, the changes of local mech. properties at the surface of polymer plaques were characterized using microindentation hardness testing (MHI), and the surface morphol. changes were studied by light and/or SEM. All methods are in accordance with the conclusion that the natural phenolic stabilizer CAT exhibited pro-oxidant activity during accelerated photooxidation of both polymers, i.e. higher concentration of oxidation products, bigger changes of local mech. properties and/or more microcracks on the exposed surfaces in comparison with non-stabilized systems and systems stabilized with Tin770.

Polymer Degradation and Stability published new progress about Antioxidants. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, HPLC of Formula: 52829-07-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Nakatani, Hisayuki published the artcileNovel Recycling System of Polystyrene Water Debris with Polymer Photocatalyst and Thermal Treatment, COA of Formula: C28H52N2O4, the main research area is polystyrene hindered amine light stabilizer polymer photocatalyst thermal treatment.

A poly(styrene-block-acrylic acid) containing TiO2 gel (PS-b-PAA/TiO2) polymer photocatalyst had the same d. as PS and could provoke photocatalytic activity to PS particles in water. It showed photocatalytic activity to a PS containing a N-H type hindered amine light stabilizer (PS/LA-77) in water under the UV irradiation The mol. weight decrease was ca. 10%, showing that a weaker light source and different kind of hindered amine light stabilizer (HALS) should be employed. The phthalocyanine modified photocatalyst had the activity under visible light irradiation In addition, a N-OR type HALS (LA-81) loading worked as radical scavenger, showing that the PS autoxidation was certainly controlled. After the 144 h irradiation, the mol. weight was drastically decreased with the increases of heating temperature and time. When the heat treatment was performed by the enclosed sample with the aluminum foil, the mol. weight change behavior was considerably different between the PS and PS/LA-81. The difference was due to the chain scission mechanism. The intra-alkyl radical production in PS chain allowed controlling mol. weight by the heat treatment.

Journal of Polymers and the Environment published new progress about Autoxidation. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, COA of Formula: C28H52N2O4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wong, Siu Wai published the artcileDevelopment of [18F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease, HPLC of Formula: 73874-95-0, the main research area is neuroinflammatory disease MER tyrosine kinase 18F MIPS15692 radiotracer; Autoradiography; CNS radiotracer; MER tyrosine Kinase; Multiple sclerosis; Positron emission tomography; X-ray crystallography.

MER tyrosine kinase (MERTK) upregulation is associated with M2 polarization of microglia, which plays a vital role in neuroregeneration following damage induced by neuroinflammatory diseases such as multiple sclerosis (MS). Therefore, a radiotracer specific for MERTK could be of great utility in the clin. management of MS, for the detection and differentiation of neuroregenerative and neurodegenerative processes. This study aimed to develop an [18F] ligand with high affinity and selectivity for MERTK as a potential positron emission tomog. (PET) radiotracer. MIPS15691 and MIPS15692 were synthesized and kinase assays were utilized to determine potency and selectivity for MERTK. Both compounds were shown to be potent against MERTK, with resp. IC50 values of 4.6 nM and 4.0 nM, and were also MERTK-selective. Plasma and brain pharmacokinetics were measured in mice and led to selection of MIPS15692 over MIPS15691. X-ray crystallog. was used to visualize how MIPS15692 is recognized by the enzyme. [18F]MIPS15692 was synthesized using an automated iPHASE FlexLab module, with a molar activity (Am) of 49 ± 26 GBq/μmol. The radiochem. purity of [18F]MIPS15692 was >99% and the decay-corrected radiochem. yields (RCYs) were determined as 2.45 ± 0.85%. Brain MERTK protein d. was measured by a saturation binding assay in the brain slices of a cuprizone mouse model of MS. High levels of specific binding of [18F]MIPS15692 to MERTK were found, especially in the corpus callosum/hippocampus (CC/HC). The in vivo PET imaging study of [18F]MIPS15692 suggested that its neuroPK is sub-optimal for clin. use. Current efforts are underway to optimize the neuroPK of our next generation PET radiotracers for maximal in vivo utility.

European Journal of Medicinal Chemistry published new progress about Blood plasma. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, HPLC of Formula: 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Tomoda, Shuji published the artcileOrigin of π-facial diastereoselection in hydride reduction of piperidones. The importance of ground-state effects, Recommanded Product: 3-Methylpiperidin-4-one, the main research area is facial stereoselectivity hydride reduction piperidinone FMO steric effect.

The exterior frontier orbital extension model (the EFOE Model) strongly suggested that the ground-state conformation (steric effects) and the anisotropic frontier orbital (LUMO) extension over π-faces may be the origin of the π-facial diastereoselection in hydride reductions of substituted piperidones.

Chemistry Letters published new progress about Conformation. 5773-58-0 belongs to class piperidines, name is 3-Methylpiperidin-4-one, and the molecular formula is C6H11NO, Recommanded Product: 3-Methylpiperidin-4-one.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Pasqualetto, Gaia published the artcileLigand-based rational design, synthesis and evaluation of novel potential chemical chaperones for opsin, Recommanded Product: tert-Butyl piperidin-4-ylcarbamate, the main research area is rhodopsin binding site chromophore preparation chem chaperone opsin; cyclohexene preparation rhodopsin binding site chromophore chem chaperone opsin; Molecular modelling; Rhodopsin; Severe inherited blinding diseases; Small-molecule agents; Synthetic organic chemistry.

Inherited blinding diseases retinitis pigmentosa (RP) and a subset of Leber’s congenital amaurosis (LCA) are caused by the misfolding and mistrafficking of rhodopsin mols., which aggregate and accumulate in the endoplasmic reticulum (ER), leading to photoreceptor cell death. One potential therapeutic strategy to prevent the loss of photoreceptors in these conditions is to identify opsin-binding compounds that act as chem. chaperones for opsin, aiding its proper folding and trafficking to the outer cell membrane. Aiming to identify novel compounds with such effect, a rational ligand-based approach was applied to the structure of the visual pigment chromophore, 11-cis-retinal, and its locked analog 11-cis-6mr-retinal. Following mol. docking studies on the main chromophore binding site of rhodopsin, 49 novel compounds, e.g., I, were synthesized according to optimized one-to seven-step synthetic routes. These agents were evaluated for their ability to compete for the chromophore binding site of opsin, and their capacity to increase the trafficking of the P23H opsin mutant from the ER to the cell membrane. Different new mols. displayed an effect in at least one assay, acting either as chem. chaperones or as stabilizers of the 9-cis-retinal-rhodopsin complex. These compounds could provide the basis to develop novel therapeutics for RP and LCA.

European Journal of Medicinal Chemistry published new progress about Cytotoxicity. 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