Category: 112-63-0

La Rosa, Francesca; Zoia, Chiara Paola; Bazzini, Chiara; Bolognini, Alessandra; Saresella, Marina; Conti, Elisa; Ferrarese, Carlo; Piancone, Federica; Marventano, Ivana; Galimberti, Daniela; Fenoglio, Chiara; Scarpini, Elio; Clerici, Mario published the artcile< Modulation of MAPK- and PI3/AKT-Dependent Autophagy Signaling by Stavudine (D4T) in PBMC of Alzheimer's Disease Patients>, Application of C19H34O2, the main research area is ERK; NLRP3-inflammasome; amyloid-β; caspase-3 and Bcl2; neuroinflammation; p38; p70S6K and CREB phosphorylation.

Background: Aβ42 deposition plays a pivotal role in AD pathogenesis by inducing the activation of microglial cells and neuroinflammation. This process is antagonized by microglia-mediated clearance of Aβ plaques. Activation of the NLRP3 inflammasome is involved in neuroinflammation and in the impairments of Aβ-plaque clearance. On the other hand, stavudine (D4T) downregulates the NLRP3 inflammasome and stimulates autophagy-mediated Aβ-clearing in a THP-1-derived macrophages. Methods: We explored the effect of D4T on Aβ autophagy in PBMC from AD patients that were primed with LPS and stimulated with Aβ oligomers in the absence/presence of D4T. We analyzed the NLRP3 activity by measuring NLRP3-ASC complex formation by AMNIS FlowSight and pro-inflammatory cytokine (IL-1β, IL-18 and Caspase-1) production by ELISA. The phosphorylation status of p38, ERK, AKT, p70, and the protein expression of CREB, LAMP2A, beclin-1, Caspase-3 and Bcl2 were analyzed by Western blot. Results: Data showed that D4T: (1) downregulates NLRP3 inflammasome activation and the production of down-stream pro-inflammatory cytokines in PBMC; (2) stimulates the phosphorylation of AKT, ERK and p70 as well as LAMP2A, beclin-1 and Bcl2 expression and reduces Caspase-3 expression, suggesting an effect of this compound on autophagy; (3) increases phospho-CREB, which is a downstream target of p-ERK and p-AKT, inducing anti-inflammatory cytokine production and resulting in a possible decrease of Aβ-mediated cytotoxicity; and (4) reduces the phosphorylation of p38, a protein involved in the production of pro-inflammatory cytokines and tau hyperphosphorylation. Conclusions: D4T reduces the activation of the NLRP3 inflammasome, and it might stimulate autophagy as well as the mol. mechanism that modulates Aβ cytotoxicity, and D4T might reduce inflammation in the cells of AD patients. It could be very interesting to check the possible beneficial effects of D4T in the clin. scenario.

Cells published new progress about 112-63-0. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Kuo, Elizabeth A.; Hambleton, Philip T.; Kay, David P.; Evans, Phillip L.; Matharu, Saroop S.; Little, Edward; McDowall, Neil; Jones, C. Beth; Hedgecock, Charles J. R. published the artcile< Synthesis, Structure-Activity Relationships, and Pharmacokinetic Properties of Dihydroorotate Dehydrogenase Inhibitors: 2-Cyano-3-cyclopropyl-3-hydroxy- N-[3'-methyl-4'-(trifluoromethyl)phenyl]propenamide and Related Compounds>, Application of C19H34O2, the main research area is immunosuppressant leflunomide metabolite analog preparation activity; dihydroorotate dehydrogenase inhibition leflunomide metabolite analog; arthritis inhibition leflunomide metabolite analog structure.

The active, ring-opened metabolite of the novel immunosuppressive agent leflunomide has been shown to inhibit the enzyme dihydroorotate dehydrogenase (DHODH). This enzyme catalyzes the fourth step in de novo pyrimidine biosynthesis. A series of analogs of the leflunomide metabolite have been synthesized. Their in vivo biol. activity determined in rat and mouse delayed type hypersensitivity has been found to correlate well with their in vitro DHODH potency. The most promising compound has shown activity in rat and mouse collagen (II)-induced arthritis models (ED50 = 2 and 31 mg/kg, resp.) and has shown a shorter half-life in man when compared with leflunomide. Clin. studies in rheumatoid arthritis are in progress.

Journal of Medicinal Chemistry published new progress about Antiarthritics. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Sandeep, Anjamkudy; Praveen, Vakayil K.; Shankar Rao, D. S.; Krishna Prasad, S.; Ajayaghosh, Ayyappanpillai published the artcile< Transforming a C3-Symmetrical Liquid Crystal to a π-Gelator by Alkoxy Chain Variation>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is self assembly columnar liquid crystal gelation.

Rational understanding of the structural features involving different noncovalent interactions is necessary to design a liquid crystal (LC) or an organogelator. Herein, we report the effect of the number and positions of alkoxy chains on the self-assembly induced phys. properties of a few π-conjugated mols. For this purpose, we designed and synthesized three C3-sym. mols. based on oligo(p-phenylenevinylene), C3OPV1-3. The self-assembly properties of these mols. are studied in the solid and solution states. All of the three mols. follow the isodesmic self-assembly pathway. Upon cooling from isotropic melt, C3OPV1 having nine alkoxy chains (-OC12H25) formed a columnar phase with two-dimensional rectangular lattice and retained the LC phase even at room temperature Interestingly, when one of the -OC12H25 groups from each of the end benzene rings is knocked out, the resultant mol., C3OPV2 lost the LC property, however, transformed as a gelator in toluene and n-decane. Surprisingly, when the -OC12H25 group from the middle position is removed, the resultant mol. C3OPV3 failed to form either the LC or the gel phases.

ACS Omega published new progress about Fluorescence. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Dubowchik, Gene M.; Michne, Jodi A.; Zuev, Dmitry; Schwartz, Wendy; Scola, Paul M.; James, Clint A.; Ruediger, Edward H.; Pin, Sokhom S.; Burris, Kevin D.; Balanda, Lynn A.; Gao, Qi; Wu, Dedong; Fung, Lawrence; Fiedler, Tracey; Browman, Kaitlin E.; Taber, Matthew T.; Zhang, Jie published the artcile< 2-Arylaminothiazoles as high-affinity corticotropin-Releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy>, Electric Literature of 112-63-0, the main research area is antidepressant thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; structure activity antidepressant anxiolytic thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; anxiolytic thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; corticotropin releasing factor receptor thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; human antidepressant thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation.

2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF1R) antagonists that are prepared in three steps in good overall yields. Herein, binding SAR as well as anxiolytic activity of an exemplary compound, N-(cyclopropylmethyl)-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-4-(trifluoromethyl)-5-thiazolemethanamine (I), in a mouse canopy model were reported. Other compounds thus prepared and tested included N-(cyclopropylmethyl)-4-methyl-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-5-thiazolecarboxamide, N,N-bis(2-methoxyethyl)-4-methyl-2-[(2,4,6-trichlorophenyl)amino]-5-thiazolecarboxamide, 2-[(2-chloro-4,6-dimethylphenyl)methylamino]-N-(cyclopropylmethyl)-N-propyl-4-(trifluoromethyl)-5-thiazolemethanamine, 2-[(2-chloro-4,6-dimethylphenyl)amino]-N-(cyclopropylmethyl)-N-propyl-4-(trifluoromethyl)-5-thiazolemethanamine. The activity of I was compared to that of an analog, N-(cyclopropylmethyl)-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-4-(trifluoromethyl)-5-oxazolemethanamine.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidepressants. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Saigal, Neil; Pichika, Rama; Easwaramoorthy, Balasubramaniam; Collins, Daphne; Christian, Bradley T.; Shi, Bingzhi; Narayanan, Tanjore K.; Potkin, Steven G.; Mukherjee, Jogeshwar published the artcile< Synthesis and biologic evaluation of a novel serotonin 5-HT1A receptor radioligand, 18F-labeled mefway, in rodents and imaging by PET in a nonhuman primate>, Reference of 112-63-0, the main research area is serotonin 5HT1A receptor fluorine 18 mefway PET.

Serotonin 5-HT1A receptors have been implicated in disorders of the central nervous system and, therefore, are being studied by PET. Efforts are under way to improve in vivo stability of 5-HT1A agents currently in human use (11C-labeled N-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-(2-pyridinyl)cyclohexanecarboxamide [11C-WAY-100635]), 4-(2′-methoxyphenyl)-1-[2′-(N-2”-pyridinyl)-p-18F-fluorobenzamido]ethylpiperazine [18F-MPPF], and 18F-labeled trans-4-fluoro-N-(2-[4-(2-methoxyphenyl)piperazin-1-yl)ethyl]-N-(2-pyridyl)cyclohexanecarboxamide) [18F-FCWAY]. We have synthesized N-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(4-18F-fluoromethylcyclohexane)carboxamide (18F-mefway), which contains a 18F on a primary carbon to make the compound more stable to defluorination. Methods: Radiosynthesis of 18F-mefway was performed in a single tosylate for 18F-fluoride exchange. In vitro binding studies on rat brain slices using 18F-mefway were read on a phosphor imager. Monkey PET studies were performed on a whole-body PET scanner. Results: Binding affinity (inhibitory concentration of 50% [IC50]) of mefway was 26 nmol/L and was comparable to that of WAY-100635, 23 nmol/L. Yields of 18F-mefway were 20%-30% in specific activities of 74-111 GBq/μmol at the end of synthesis. In vitro binding of 18F-mefway in the hippocampus (Hp), colliculus (Co), cortex (Ctx), and other brain regions-with limited binding in the cerebellum (Cer)-was observed, with ratios of Hp/Cer = 82.3, Co/Cer = 45.8, and Ctx/Cer = 40. Serotonin displaced 18F-mefway from various brain regions with IC50 values in the range of 169-243 nmol/L. PET studies in a rhesus monkey showed 18F-mefway binding in the fontal cortex (FC), temporal cortex (TC) including hippocampus, raphe (Rp), and other brain regions, with ratios of FC/Cer = 9.0, TC/Cer = 10, and Rp/Cer = 3.3. Plasma anal. indicated the presence of approx. 30% of 18F-mefway at 150-180 min after injection. Conclusion: The high ratios in specific brain regions such as the hippocampus suggest that 18F-mefway has potential as a PET agent for 5HT1A receptors.

Journal of Nuclear Medicine published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zenouz, A. Moshtaghi; Allahverdi, S.; Raissossadat Q., M.; Sadeghi Sh., Q. published the artcile< Synthesis of the C-2 functionalized 1,4-dihydropyridines>, Application In Synthesis of 112-63-0, the main research area is methyl pyridine bromination; bromomethyl pyridine preparation reaction thiourea; isothiuronium salt pyridine preparation reaction methyl iodide; sulfide methyl pyridine preparation; dithiane reaction bromomethyl pyridine; dithio acetal preparation.

Unsym. 1,4-dihydropyridine esters were synthesized from the sym. precursor 2,6-dimethylpyridine derivative through the intermediacy of 2-bromomethyl derivative 2-bromomethyl-6-methylpyridine derivative Then reaction of isothiuronium salt of pyridine derivative with electrophilic specie, methyl-iodide, in the presence of base produced S-methylated pyridine derivative Reaction of the dibrominated pyridine derivative with lithium salt of 1,3-dithiane led to the formation of dithio acetal of pyridine derivative

Asian Journal of Chemistry published new progress about 112-63-0. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wuensch, Bernhard; Nerding, Sven published the artcile< A facile and regioselective synthesis of donor-substituted 2-(2-halophenyl)acetaldehyde acetals>, HPLC of Formula: 112-63-0, the main research area is regioselective preparation donor substituted halophenylacetaldehyde acetal.

Starting from vanillin a facile and high yielding procedure for the preparation of the donor substituted (2-bromophenyl)- and (2-iodophenyl)-acetaldehyde acetals I [R = Br (II), I (III)] is described. Homologation of O-benzylvanillin to obtain the phenylacetaldehyde acetal I [R = H(IV)]succeeds by Wittig reaction with the Ph3P+CH2OMe Cl- and subsequent addition of methanol. IV is brominated with pyridinium bromide perbromide in methanol to yield the bromo acetal II in 65% yield from vanillin. Iodination of IV with iodine and iodic acid leads to the iodo acetal III.

Archiv der Pharmazie (Weinheim, Germany) published new progress about Acetals Role: SPN (Synthetic Preparation), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, HPLC of Formula: 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ramakrishna Pillai, Jayachithra; Wali, Adil Farooq; Menezes, Godfred Antony; Rehman, Muneeb U.; Wani, Tanveer A.; Arafah, Azher; Zargar, Seema; Mir, Tahir Maqbool published the artcile< Chemical Composition Analysis, Cytotoxic, Antimicrobial and Antioxidant Activities of Physalis angulata L.: A Comparative Study of Leaves and Fruit>, Related Products of 112-63-0, the main research area is Physalis leaf fruit phytochem antimicrobial antioxidant cytotoxicity; DLD-1; HeLa; MCF-7; Physalis angulata; Solanaceae; antioxidant activity; cytotoxic activity.

Physalis angulata L. belongs to the family Solanaceae and is distributed throughout the tropical and subtropical regions. Physalis angulata leaf and fruit extracts were assessed for in vitro anticancer, antioxidant activity, and total phenolic and flavonoid content. The GC-MS technique investigated the chem. composition and structure of bioactive chems. reported in extracts The anticancer activity results revealed a decrease in the percentage of anticancer cells′ viability in a concentration- and time-dependent way. We also noticed morphol. alterations in the cells, which we believe are related to Physalis angulata extracts Under light microscopy, we observed that as the concentration of ethanolic extract (fruit and leaves) treated HeLa cells increased, the number of cells began to decrease.

Molecules published new progress about Alkaloids Role: PAC (Pharmacological Activity), THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Redjeb, Youcef; Kaabeche-Djerafi, Khatima; Stoppato, Anna; Benato, Alberto published the artcile< The IRC-PD Tool: A Code to Design Steam and Organic Waste Heat Recovery Units>, Quality Control of 112-63-0, the main research area is steam organic waste Rankine cycle heat recovery design.

The Algerian economy and electricity generation sector are strongly dependent on fossil fuels. Over 93% of Algerian exports are hydrocarbons, and approx. 90% of the generated electricity comes from natural gas power plants. However, Algeria is also a country with huge potential in terms of both renewable energy sources and industrial processes waste heat recovery. For these reasons, the government launched an ambitious program to foster renewable energy sources and industrial energy efficiency. In this context, steam and organic Rankine cycles could play a crucial role; however, there is a need for reliable and time-efficient optimization tools that take into account tech., economic, environmental, and safety aspects. For this purpose, the authors built a math. tool able to optimize both steam and organic Rankine units. The tool, called Improved Rankine Cycle Plant Designer, was developed in MATLAB environment, uses the Genetic Algorithm toolbox, acquires the fluids thermophys. properties from CoolProp and REFPROP databases, while the safety information is derived from the ASHRAE database. The tool, designed to support the development of both RES and industrial processes waste heat recovery, could perform single or multi-objective optimizations of the steam Rankine cycle layout and of a multiple set of organic Rankine cycle configurations, including the ones which adopt a water or an oil thermal loop. In the case of the ORC unit, the working fluid is selected among more than 120 pure fluids and their mixtures The turbines’ design parameters and the adoption of a water- or an air-cooled condenser are also optimization results. To facilitate the plant layout and working fluid selection, the economic anal. is performed to better evaluate the plant economic feasibility after the thermodn. optimization of the cycle. Considering the willingness of moving from a fossil to a RES-based economy, there is a need for adopting plants using low environmental impact working fluids. However, because ORC fluids are subjected to environmental and safety issues, as well as phase out, the code also computes the Total Equivalent Warming Impact, provides safety information using the ASHRAE database, and displays an alert if the organic substance is phased out or is going to be banned. To show the tool’s potentialities and improve the knowledge on waste heat recovery in bio-gas plants, the authors selected an in-operation facility in which the waste heat is released by a 1 MWel internal combustion engine as the test case. The optimization outcomes reveal that the tech., economic, environmental, and safety performance can be achieved adopting the organic Rankine cycle recuperative configuration. The unit, which adopts Benzene as working fluid, needs to be decoupled from the heat source by means of an oil thermal loop. This optimized solution guarantees to boost the electricity production of the bio-gas facility up to 15%.

Energies (Basel, Switzerland) published new progress about Air. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Quality Control of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Chernov, Alexandr N.; Filatenkova, Tatiana A.; Glushakov, Ruslan I.; Buntovskaya, Alexandra S.; Alaverdian, Diana A.; Tsapieva, Anna N.; Kim, Alexandr V.; Fedorov, Evgeniy V.; Skliar, Sofia S.; Matsko, Marina V.; Galimova, Elvira S.; Shamova, Olga V. published the artcile< Anticancer Effect of Cathelicidin LL-37, Protegrin PG-1, Nerve Growth Factor NGF, and Temozolomide: Impact on the Mitochondrial Metabolism, Clonogenic Potential, and Migration of Human U251 Glioma Cells>, Category: esters-buliding-blocks, the main research area is ECAR; OCR; cathelicidin LL-37; clonogenicity; human glioma U251; metabolism of mitochondria; migration; nerve growth factor NGF; protegrin PG-1; temozolomide.

Glioblastoma (GBM) is one of the most aggressive and lethal malignancy of the central nervous system. Temozolomide is the standard of care for gliomas, frequently results in resistance to drug and tumor recurrence. Therefore, further research is required for the development of effective drugs in order to guarantee specific treatments to succeed. The aim of current study was to investigate the effects of nerve growth factor (NGF), human cathelicidin (LL-37), protegrin-1 (PG-1), and temozolomide on bioenergetic function of mitochondria, clonogenicity, and migration of human U251 glioma cells. Colony formation assay was used to test the ability of the glioma cells to form colonies in vitro. The U251 glioma cells migration was evaluated using wound-healing assay. To study the mitochondrial metabolism in glioma cells we measured oxygen consumption rates (OCR) and extracellular acidification rates (ECAR) using a Seahorse XF cell Mito stress test kit and Seahorse XF cell Glycolysis stress kit, resp. We revealed that LL-37, NGF, and TMZ show strong anti-tumorigenic activity on GMB. LL-37 (4 μM), TMZ (155 μM), and NGF (7.55 x 10-3 μM) inhibited 43.9%-60.3%, 73.5%-81.3%, 66.2% the clonogenicity of glioma U251 cells for 1-2 days, resp. LL-37 (4 μM), and NGF (7.55 x 10-3 μM) inhibited the migration of U251 glioma cells on the third and fourth days. TMZ also inhibited the migration of human glioma U251 cells over 1-3 days. In contrast, PG-1 (16 μM) stimulated the migration of U251 glioma cells on the second, fourth, and sixth days. Anti-mitogenic and anti-migration activities of NGF, LL-37, and TMZ maybe are relation to their capacity to reduce the basal OCR, ATP-synthetase, and maximal respiration of mitochondria in human glioma U251 cells. Glycolysis, glycolytic capacity and glycolytic spare in glioma U251 cells haven’t been changed under the effect of NGF, LL-37, PG-1, and TMZ in regard to control level. Thus, LL-37 and NGF inhibit migration and clonogenicity of U251 glioma cells, which may indicate that these compounds have anti-mitogenic and anti-migration effects on human glioma cells. The study of the mechanisms of these effects may contribute in the future to the use of NGF and LL-37 as therapeutic agents for gliomas.

Molecules published new progress about 112-63-0. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics