Category: piperidines

Ogasawara, Daisuke published the artcileDiscovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12), Computed Properties of 73874-95-0, the main research area is lysophosphatidylserine lipase hydrolase domain 12 ABHD12 inhibitor.

ABHD12 is a membrane-bound hydrolytic enzyme that acts on the lysophosphatidylserine (lyso-PS) and lysophosphatidylinositol (lyso-PI) classes of immunomodulatory lipids. Human and mouse genetic studies point to a key role for the ABHD12-(lyso)-PS/PI pathway in regulating (neuro)immunol. functions in both the central nervous system and periphery. Selective inhibitors of ABHD12 would offer valuable pharmacol. probes to complement genetic models of ABHD12-regulated (lyso)-PS/PI metabolism and signaling. Here, we provide a detailed description of the discovery and activity-based protein profiling (ABPP) guided optimization of reversible thiourea inhibitors of ABHD12 that culminated in the identification of DO264 as a potent, selective, and in vivo active ABHD12 inhibitor. We also show that DO264, but not a structurally related inactive control probe (S)-DO271, augments inflammatory cytokine production from human THP-1 macrophage cells. The in vitro and in vivo properties of DO264 designate this compound as a suitable chem. probe for studying the biol. functions of ABHD12-(lyso)-PS/PI pathways.

Journal of Medicinal Chemistry published new progress about Crystal structure. 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

Modranka, Jakub published the artcileSynthesis and Structure-Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X, Formula: C10H20N2O2, the main research area is benzooxazinone analog preparation Mycobacterial thymidylate synthase tuberculosis; antibiotics; benzo[b][1,4]oxazine; drug discovery; tuberculosis.

Since the discovery of a flavin-dependent thymidylate synthase (ThyX or FDTS) that is absent in humans but crucial for DNA biosynthesis in a diverse group of pathogens, the enzyme has been pursued for the development of new antibacterial agents against Mycobacterium tuberculosis, the causative agent of the widespread infectious disease tuberculosis (TB). In response to a growing need for more effective anti-TB drugs, we have built upon our previous screening efforts and report herein an optimization campaign of a novel series of inhibitors with a unique inhibition profile. The inhibitors display competitive inhibition toward the methylene tetrahydrofolate cofactor of ThyX, enabling us to generate a model of the compounds bound to their target, thus offering insight into their structure-activity relationships.

ChemMedChem published new progress about Enzyme inhibitors. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takimoto, Ken published the artcileExploring stabilizer formulations for light-induced yellowing of polystyrene by high-throughput experimentation and machine learning, Safety of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is photo induced yellowing inhibition polystyrene stabilizer formulation machine learning.

In this study, a high-throughput exptl. protocol was established for yellowing inhibition of transparent plastics on the basis of solution film casting on microplates and UV/visible (UV/Vis) spectroscopic evaluation using a microplate reader. A combination of the protocol and a genetic algorithm realized a large-scale exploration of stabilizer formulations that consist of com. available hindered amine stabilizers and UV absorbers, etc. The found formulations were highly effective in inhibiting the photo-induced yellowing of polystyrene, compared to the most efficient single stabilizer at the fixed concentration The obtained data, which corresponded to seven years of aging (when sequentially acquired), were analyzed and validated based on decision tree classification, force-directed network visualization, and so on. A formulation design guideline was successfully derived that it is essential to combine as many stabilizers that are complementary and synergistic with each other as possible.

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bose, D. Subhas published the artcileBoron trifluoride promoted cleavage of benzyl carbamates, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate, the main research area is boron trifluoride promoted cleavage benzyl carbamate.

A new efficient method for the cleavage of benzyl carbamates (CBZ protective groups), e.g., I, is described that involves a hard acid (BF3.OEt2)-soft nucleophile (EtSH) system. Unlike other available methods, this combination avoids the reduction of olefins, acetylenes, imines, halides and nitro groups, or the possibility of carboxylic ester hydrolysis.

Tetrahedron Letters published new progress about Protective groups. 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate.

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

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

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

Le, Chen published the artcileReclaimed water application to vegetation restoration in mining area: determination of water quality standards and optimization of moderate treatment technology, Quality Control of 52829-07-9, the main research area is water quality standard determination vegetation restoration moderate treatment technol.

Water shortage severely restricts vegetation restoration of mining area in the northwest China. Moderate treatment of reclaimed water is essential for improving the local ecol. environment. In this study, relevant water quality standards issued by the states and research results were comprehensively considered to propose a reclaimed water quality standard suitable for vegetation restoration of mining area. The available domestic sewage and mine water was moderately treated by hybrid biol. reactor system and nanofiltration membrane system, resp. The effluent quality meet the requirement of reclaimed water quality standards in this study. This study provides theor. support for vegetation restoration of mining area.

E3S Web of Conferences published new progress about Chemical oxygen demand. 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

Xu, Xi published the artcileDiscovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles, COA of Formula: C10H20N2O2, the main research area is piperidinamine linker aromatic heterocycle preparation design GLS1 glutaminase inhibitor; glutaminase GLS1 allosteric inhibitor SAR metabolic stability antitumor; 4-Piperidinamine; Allosteric inhibitors; GLS1; Glutaminase 1; Glutamine metabolism.

Glutaminase 1 (GLS1) is overexpressed in multiple types of malignant tumors and is viewed as a promising target in cancer therapy. Thus, the discovery for small-mol. GLS1 inhibitors is urgent. Based on the authors’ previous study of compound I, a potent GLS1 allosteric inhibitor yet with a limited metabolic stability, a structure-based optimization was carried out, with a series of novel GLS1 allosteric inhibitors rationally designed, synthesized and biol. evaluated. Such endeavor has culminated in the identification of compound II, a promising GLS1 allosteric inhibitor with a 4-piperidinamine linker and aromatic heterocycles. Compound II displayed robust GLS1 binding affinity, superior liver microsome metabolic stability, and moderate anti-tumor activity (TGI: 47.5%) in HCT116 xenograft model with no considerable toxicity in vivo. The mechanism underlying the anti-proliferative effect of compound II on HCT116 cells was studied, revealing that the compound blocked the glutamine metabolism, induced the production of ROS, and triggered apoptosis. These findings merit further investigation of compound II as a targeted cancer therapeutic.

European Journal of Medicinal Chemistry published new progress about Allosteric modulators. 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

Malakoutikhah, Morteza published the artcileN-Methyl Phenylalanine-Rich Peptides as Highly Versatile Blood-Brain Barrier Shuttles, HPLC of Formula: 158922-07-7, the main research area is blood brain barrier delivery peptide drug.

Here we studied the capacity of N-MePhe-(N-MePhe)3-CONH2, Cha-(N-MePhe)3-CONH2, and 2Nal-(N-MePhe)3-CONH2 to carry various drugs (cargos) in in vitro blood-brain barrier (BBB) models in order to determine the versatility of these peptides as BBB-shuttles for drug delivery to the brain. Using SPPS, the peptides were coupled to GABA, Nip, and ALA to examine their passive BBB permeation by means of PAMPA and their lipophilicity by IAMC. Unaided, these nonpermeating drugs alone did not cross the PAMPA barrier and the BBB passively; however, the peptides tested as potential BBB shuttles transferred them by passive transfer through the PAMPA phospholipid. The permeability of peptides that showed the highest permeability in PAMPA, and Ac-N-MePhe-(N-MePhe)3-CONH2 as the parent peptide was also examined in bovine brain microvessel endothelial cells (BBMECs). These peptide-based BBB shuttles open up the possibility to overcome the formidable obstacle of the BBB, thereby achieving drug delivery to the brain.

Journal of Medicinal Chemistry published new progress about Biological permeation. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, HPLC of Formula: 158922-07-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem