Month: November 2022

Giancola, JoLynn B. published the artcileStructure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability, Synthetic Route of 73874-95-0, the main research area is aminopiperidine piperidine amine preparation dopamine transporter SAR; Atypical dopamine uptake inhibitors; Cocaine; DAT; Modafinil; NET; Psychostimulant use disorders; SERT; Sigma receptors.

The bioisosteric substitutions of the piperazine ring were explored with a series of aminopiperidines and piperidine amines wherein compounds with either a terminal tertiary amine or amide were synthesized. Several lead compounds showed high to moderate DAT affinities and metabolic stability in rat liver microsomes. N-(2-((bis(4-fluorophenyl)methyl)sulfinyl)ethyl)-1-(4-fluorobenzyl)piperidin-4-amine (DAT Ki = 50.6 nM), I [R= F] (DAT Ki = 77.2 nM) and II [X1=X2= F] (DAT Ki = 30.0 nM) produced only minimal stimulation of ambulatory activity in mice, compared to cocaine, suggesting an atypical DAT inhibitor profile.

European Journal of Medicinal Chemistry published new progress about Alkylation. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zeng, Xiaojun published the artcileCopper-Catalyzed Decarboxylative Difluoromethylation, HPLC of Formula: 158922-07-7, the main research area is copper catalyzed decarboxylative difluoromethylation; difluoromethylation aliphatic carboxylic acid radical mechanism.

We report herein a highly efficient Cu-catalyzed protocol for the conversion of aliphatic carboxylic acids to the corresponding difluoromethylated analogs. This robust, operationally simple and scalable protocol tolerates a variety of functional groups and can convert a diverse array of acid-containing complex mols. to the alkyl-CF2H products. Mechanistic studies support the involvement of alkyl radicals.

Journal of the American Chemical Society published new progress about Alkylation. 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

Valentukeviciene, Marina published the artcileFluoride Removal from Groundwater by Technological Process Optimization, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is fluoride removal groundwater technol process optimization.

Fluoride removal from aqueous solutions was studied using nanofiltration and sorption techniques which have always been best key ways to deal with water contaminated by fluoride. In this presented work, we were firstly interested on fluoridated rejected water overcoming the drawback of RO membrane process of groundwater treatment plant in Baltic region (Kretinga, Lithuania). Opoka sorbent has shown effective results of fluoride sorption with efficiency higher than 77%. In order to understand the sorption phenomenon and to validate the results obtained, we have applied exptl. data on Freundlich and Langmuir isotherms which allow us to determine isotherms parameters (KF; 1/n and KL; qmax) and to confirm the experiment Because of the unacceptable tariff of drinking water treated by RO, defluoridation with nanofiltration method is proposed in this study as a solution which can replace reverse osmosis technique. For that, tests of nanofiltration for fluoride removal were carried out at laboratory scale by using nanofiltration flat sheet membranes (NF270 and NF90).

Ecological Chemistry and Engineering S published new progress about Adsorption. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Lin, Yi-Li published the artcileUsing in situ modification to enhance organic fouling resistance and rejection of pharmaceutical and personal care products in a thin-film composite nanofiltration membrane, HPLC of Formula: 52829-07-9, the main research area is NF90 hydroxyethyl sulfopropyl methacrylate potassium personal care product antifouling; Adsorption; Antifouling; In situ modification; Modified Hermia model; Nanofiltration; Pharmaceutical and personal care products (PPCPs); Radical graft polymerization.

A com. available nanofiltration membrane, NF90, was modified using an in situ concentration polarization-enhanced radical graft polymerization method to improve the organic fouling resistance as well as the removal of pharmaceutical and personal care products (PPCPs), including ibuprofen (IBU), carbamazepine, sulfadiazine, sulfamethoxazole, sulfamethazine, and triclosan (TRI). 3-Sulfopropyl methacrylate potassium salt (SPM) and 2-hydroxyethyl methacrylate (HEMA) were used in various dosages for surface modification, and the extent of membrane modifications was quantified based on the degree of grafting. The modified NF90 exhibited a 15-40% lower flux during humic acid (HA) fouling and 25% greater NaCl rejection compared with the virgin membrane. PPCP rejection in the modified NF90 membranes before and after HA fouling was 20-45% and 5-20% greater, resp., compared with that of the virgin membrane. Both SPM and HEMA increased the hydrophilicity of NF90 by decreasing contact angles. SEM revealed lower amounts of foulants on the modified NF90 than on the virgin membrane. The main fouling mechanism for virgin NF90 was gel layer formation and those for modified NF90 were complete and intermediate blocking. Therefore, the modification of NF90 was effective for controlling organic fouling and strongly rejecting PPCPs.

Environmental Science and Pollution Research published new progress about Adsorption. 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

Ishida, Akiharu published the artcileDiscovery and SAR Studies of Orally Active Somatostatin Receptor Subtype-2 (SSTR2) Agonists for the Treatment of Acromegaly, Synthetic Route of 73874-95-0, the main research area is acromegaly somatostatin SSTR2 GPCR acromegaly nonpeptidic orally active SAR; GPCR; SSTR2; Somatostatin; acromegaly; nonpeptidic; orally active.

Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by i.v. injection with cyclic peptide drugs that activate somatostatin receptor subtype 2 (SSTR2). Here, novel nonpeptidic, small-mol., and orally active SSTR2 agonists were identified from a hit compound (13). Pharmacophore studies enabled scaffold hopping to obtain a unique 3,4,5-trisubstituted pyridine motif. Further optimization conferred potent SSTR2 agonistic activity and metabolic stability. Several compounds were evaluated and these showed good oral pharmacokinetic profiles in rats, and one representative compound (25)(I) showed highly potent inhibition of growth hormone secretion induced by growth hormone-releasing hormone in rats. Based on these results, 25 was identified as a promising lead for further optimization. A structure-activity relationship (SAR) study and the metabolic stability data for this compound are also described.

ACS Chemical Neuroscience published new progress about Acromegaly. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rus, Anika Zafiah M. published the artcileDeterioration rate of renewable polyurethanes composites prior to ultra violet irradiation exposure, Application of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is polyurethane composite preparation UV irradiation deterioration.

Polyurethanes (PU’s) made from renewable and sustainable materials are one of the most important groups of polymers because of their versatility with wide range of grades, densities and stiffness. In this project, polymers based on renewable materials such as rapeseed (RS) and sunflower oil (SF) were synthesized and cross-linked to form polyurethanes. The effect of prolonged exposure up to 1000 h upon UVB light, in general promotes photodegradation for both RS and SF-based polyurethanes, both neat and also composites loaded with TiO2. The addition of 10% Degussa P25 TiO2 pigment, gives the greater degradation while PUs loaded with 5% Kronos 2220 show the slowest rates of degradation due to the effect of the coating of this pigment. The photostabilizer Tinuvin 770 offers high protection from UVB, thus lead the combination of Tinuvin 770 with Degussa P25 promotes the highest protection from UVB exposure. Moreover, addition of Tinuvin 770 at the stage of preparation of the PUs also greatly reduced the undesirable yellow coloration prevalent during PU synthesis.

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wu, Lei published the artcileBromination-induced spirocyclization of rhodamine dyes affording a FRET-based ratiometric fluorescent probe for visualization of hypobromous acid (HOBr) in live cells and zebrafish, Synthetic Route of 73874-95-0, the main research area is rhodamine dye fluorescent probe hypobromous acid zebrafish bromination spirocyclization.

Hypobromous acid (HOBr) has been implicated in many physiol. and pathol. conditions. Therefore, real-time monitoring of HOBr fluctuations in biosystem plays a key role for understanding pathophysiol. processes. To date, it remains a challenge to design fluorescent probes specific toward HOBr, because HOBr and HOCl have similar chem. properties and the former has a relatively lower concentration in comparison with the former in living system. Herein, a Forster resonance energy transfer (FRET)-based ratiometric fluorescent HOBr probe (Cou-RhB) was developed. The probe consists of a coumarin donor and a rhodamine acceptor. Upon treatment of Cou-RhB with HOBr, the electrophilic bromination of xanthene ring occurs, which shifts the equilibrium of rhodamine from the highly absorbing and fluorescent zwitterion form to the colorless and non-fluorescent spirolactone form, thus decreasing the FRET efficiency within the probe. The above reaction affords a large emission wavelength shift (ca. 89 nm), and ratiometric sensing of HOBr can be realized by measuring the ratio of coumarin- to rhodamine-type intensities (I491/I580). Cou-RhB responds to HOBr with a fast kinetics (∼ 10 s), high sensitivity and excellent specificity and has been applied for ratiometric imaging of HOBr inside live cells and zebrafish.

Sensors and Actuators, B: Chemical published new progress about Absorption. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liu, Wenjie published the artcileDesign, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer’s disease, SDS of cas: 73874-95-0, the main research area is coumarin preparation docking antitumor enzyme inhibitor ADME Alzheimer disease; AChE; Alzheimer’s disease; BACE1; Coumarin; GSK-3β.

Herein, a series of novel coumarin derivatives such as I and II [R = 3-pyridinyl, 4-pyridinyl, 2-F-4-pyridinyl, 6-F-3-pyridinyl, 4-FC6H4, 2-(cyclopropylcarbonylamino)-4-pyridinyl, 2-(benzoylamino)-4-pyridinyl] was explored, synthesized, and assessed their inhibitory effects on cholinesterase (AChE, BuChE), GSK-3β, and BACE1. Among these compounds, compound II (R = pyridin-3-yl) displayed the multifunctional profile of targeting the AChE (IC50 = 1.313 ± 0.099μM) with a good selectivity over BuChE (SI = 24.623), GSK-3β (19.30% inhibition at 20μM), BACE1 (IC50 = 1.227 ± 0.112μM), along with moderate HepG2 cytotoxicity, SH-SY5Y cytotoxicity, low HL-7702 cytotoxicity, as well as good blood-brain barrier (BBB) permeability. Kinetic and docking studies indicated that compound II (R = pyridin-3-yl) was a competitive AChE inhibitor. Furthermore, acute toxicity experiments revealed that it was non-toxic at a dosage of 1000 mg/kg. The ADME prediction results indicate that II (R = pyridin-3-yl) has acceptable physicochem. properties. Collectively, these findings demonstrated that compound II (R = pyridin-3-yl) would be a potential multifunctional candidate for AD therapy.

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Tavares, Ines G. published the artcileIntramolecular interchromophore singlet-singlet and triplet-singlet energy transfer in a metal-free donor-acceptor emitter, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is intramol interchromophore singlet triplet energy transfer donor acceptor emitter.

In this work we demonstrate the occurrence of singlet to singlet, and triplet to singlet, intramol. energy transfer between two thiophene-comprising donors (D) and a central perylene bisimide acceptor (A) covalently linked to each other trough a linker that separates the donor and acceptor moieties in a D-A-D structure. The designed metal-free organic tandem luminophore is herein designated as ARC-1467. Energy transfer from the excited triplet state of the thiophene donor to the singlet state of the perylene bisimide acceptor is observed in solution and in solid films of ARC-1467 dispersed in polystyrene. When the perylene bisimide acceptor is directly excited, the fluorescence decays with 4.9 ns lifetime. However, upon excitation of the donor unit in the near-UV region, delayed fluorescence of perylene bisimide with 5.7 μs lifetime is distinctly observed demonstrating the occurrence of energy transfer from the triplet state of the D unit to the perylene bisimide acceptor.

Journal of Luminescence published new progress about Absorption. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liu, Qian published the artcileDesign, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is APN AKT dual inhibitor CD13 kinase antitumor polypharmacol.

Herein a novel series of APN and AKT dual inhibitors were derived from the clin. AKT inhibitor AZD5363. It was demonstrated that most compounds exhibited remarkable APN inhibitory activities with the most potent compound 8b (I) (IC50 = 0.05 ± 0.01 μM) being over 70-fold more potent than the approved APN inhibitor bestatin (IC50 = 3.64 ± 0.56 μM). The moderate AKT inhibitory potencies of target compounds were also confirmed, with 5f (II) and 5h (III) possessing AKT1 IC50 values of 0.12 and 0.27 μM, resp. More importantly, the APN IC50 values of 5f and 5h were 0.96 and 0.21 μM, resp., indicating their balanced APN and AKT dual inhibition. HUVEC tube formation assays confirmed the superior APN inhibitory activities of 5f and 5h relative to bestatin at the cellular level. Western blot anal. demonstrated that 5h could effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT.

ACS Medicinal Chemistry Letters published new progress about Drug design. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem