Day: November 16, 2022

Rathinamoorthy, R. published the artcileDisposable tri-layer masks and microfiber pollution – An experimental analysis on dry and wet state emission, Synthetic Route of 52829-07-9, the main research area is disposable trilayer mask microfiber pollution dry wet emission; Freshwater; Microfiber shedding; Polypropylene; Rubbing; Seawater; Tri-layer mask.

The use of masks as a personal protective material is the new normal in the post-pandemic. The higher use of masks triggers immediate disposal of synthetic textile fibers leading to environmental pollution. This research is aimed to analyze the level of mask-related pollution and its impact on microfiber release. Microfiber emission characteristics of the tri-layer nonwoven mask (Polypropylene-based disposable mask) are analyzed in the dry and wet stages. The individual layers of the mask and the entire mask are evaluated by subjecting them to static immersion and mech. agitation against freshwater and seawater in the wet stage. The results of the study showed a higher microfiber shedding at dry state (14,031.97-177,601.58 fibers/mask) than the wet state (2557.65-22,525.89 fibers/mask). The increased fuzz formation in the dry state than the wet state is noted as the main reason. In the case of wet state, when the freshwater and seawater are compared, both in a static and agitated state, seawater degraded the mask highly (3358.03-27,348.9 fibers/mask) than the freshwater (1757.26-17,702.86 fibers/mask). Higher salinity and d. of the seawater were noted as influencing parameters over the freshwater. When the results of naturally weathered masks are compared with the new mask, weathered masks released significantly (p < 0.05) higher amount of fibers at the evaluation stages. Similar to the new masks, the weathered masks also showed a higher amount of shedding in the dry state and presence of seawater. When the individual layers of the disposable masks were evaluated, at dry and wet states, all the layers showed a similar shedding (no significant difference between individual layers) in the case of a new mask. Whereas, after weathering, a significant amount of higher shedding (p < 0.05) is noted in the middle layer of the mask followed by the outer and inner layer. The difference in fiber composition is noted as the main reason for the strength difference of the nonwoven structure. Statistical anal. confirmed the significant impact of the natural weathering process and seawater on the microfiber shedding. Science of the Total Environment published new progress about Environmental pollution. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Synthetic Route of 52829-07-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Hamper, Bruce C. published the artcileSolid Phase Synthesis of β-Peptoids: N-Substituted β-Aminopropionic Acid Oligomers, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, the main research area is solid phase preparation peptoid combinatorial library; substituted aminopropionic acid oligomer library preparation.

A solid-phase organic synthesis method has been developed for the preparation of N-substituted-β-aminopropionic acid oligomers or β-peptoids I. Treatment of polymer-bound 4-(benzyloxy)benzyl acrylate with primary amines afforded N-substituted β-alanines. Polymer loadings and product conversions were determined by direct cleavage of resin-bound materials and measurement by 1H NMR with an internal standard The NMR method was used to establish loading of all resin-bound intermediates including acrylic acid. Acylation with acryloyl chloride followed by Michael addition of primary amines to the acrylamide allowed preparation of di-β-peptoids. By a linear set of seven reactions, trimeric N-benzyl-β-aminopropionic acid was prepared in 67% overall yield. Single-bead FT-IR microspectroscopy was used to acquire spectra of the resin bound mono-β-peptoids, di-β-peptoids, and acrylamide intermediates. A combinatorial library of defined mixtures of tri-β-peptoids was prepared by mixing equimolar amounts of the mono-β-peptoid resins and carrying them through two sequences of the acylation-Michael addition The identity of a sample mixture II (R = Me, CH2Ph, CH2CH2Ph, CH2C6H4OMe-4, allyl, CH2CHMe2, CHMeEt, CHMe2) was determined by LC-MS anal. of the cleavage product.

Journal of Organic Chemistry published new progress about Combinatorial chemistry. 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, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Dolle, Roland E. published the artcileA statistical-based approach to assessing the fidelity of combinatorial libraries encoded with electrophoric molecular tags. Development and application of tag decode-assisted single bead LC/MS analysis, COA of Formula: C21H21NO4, the main research area is statistical sampling mol tag encoded combinatorial library statine amide; combinatorial library QA method tag decoding single bead LCMS; statine peptide library preparation inhibition screening cathepsin plasmepsin.

A statistical sampling protocol is described to assess the fidelity of libraries encoded with mol. tags. The methodol., termed library QA, is based on the combined application of tag decode anal. and single bead LC/MS. The phys. existence of library compounds eluted from beads is established by comparing the mol. weight predicted by tag decode with empirical measurement. The goal of sampling is to provide information on overall library fidelity and an indication of the performance of individual library synthons. The minimal sampling size n for library QA is 10× the largest synthon set. Data are reported as proportion (p) ± lower and upper boundary (lb-ub) computed at the 95% confidence level (α = 0.05). As a practical demonstration, library QA was performed on a 25 200-member library of statine-containing peptide amides (size = 40 × 63 × 10). Sampling was conducted three times at n ∼ 630 beads per run for a total of 1902 beads. The overall proportions found for the three runs were consistent with one another: p = 84.4%, lb-ub = 81.5-87.2%; p = 83.1%, lb-ub = 80.2-85.95; and p = 84.5%, lb-ub = 81.8-87.3%, suggesting the true value of p is close to 84% compound confirmation. The performance pi of individual synthons was also computed. Corroboration of QA data with biol. screening results obtained from assaying the library against cathepsin D and plasmepsin II is discussed.

Journal of Combinatorial Chemistry published new progress about Combinatorial chemistry. 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, COA of Formula: C21H21NO4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kamakolanu, Uma Gayathri published the artcileDiscovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson’s Disease Models, SDS of cas: 73874-95-0, the main research area is piperdinylindole synthesis antiparkinson SAR nociceptin opioid receptor Parkinsons dyskinesia.

A novel series of C(3)-substituted piperdinylindoles were developed as nociceptin opioid receptor (NOP) partial agonists to explore a pharmacol. hypothesis that NOP partial agonists would afford a dual pharmacol. action of attenuating Parkinson’s disease (PD) motor symptoms and development of levodopa-induced dyskinesias. SAR around the C-3 substituents investigated effects on NOP binding, intrinsic activity, and selectivity and showed that while the C(3)-substituted indoles are selective, high affinity NOP ligands, the steric, polar, and cationic nature of the C-3 substituents affected intrinsic activity to afford partial agonists with a range of efficacies. Compounds 4, 5, and 9 with agonist efficacies between 25% and 35% significantly attenuated motor deficits in the 6-OHDA-hemilesioned rat model of PD. Further, unlike NOP antagonists, which appear to worsen dyskinesia expression, these NOP partial agonists did not attenuate or worsen dyskinesia expression. The NOP partial agonists and their SAR reported here may be useful to develop nondopaminergic treatments for PD.

Journal of Medicinal Chemistry published new progress about Antiparkinsonian agents. 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

Tiwari, Shashi B. published the artcileSynthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson’s agents, Computed Properties of 1690-74-0, the main research area is bromo dimethoxyphenyl oxadiazole preparation antiparkinson activity.

A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives, e.g., I, was prepared and their evaluation for anti-Parkinson’s activity was measured in vivo using albino rats. The result of the biol. activity studies indicated that some of the synthesized compounds have good agonistic activity on the dopamine receptors and a few of them were also found to be free from neurotoxicity. Thus these compounds might be useful ligands for studying the functional role of dopamine receptors in vivo. The high log P value of the compounds indicates that they should easily cross the blood-brain barrier (log P > 2.6).

Medicinal Chemistry Research published new progress about Antiparkinsonian agents. 1690-74-0 belongs to class piperidines, name is Methyl 1-methylpiperidine-2-carboxylate, and the molecular formula is C8H15NO2, Computed Properties of 1690-74-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Motika, Stephen E. published the artcileGram-Negative Antibiotic Active Through Inhibition of an Essential Riboswitch, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is antibiotic riboswitch ribocil.

Multidrug-resistant Gram-neg. (GN) infections for which there are few available treatment options are increasingly common. The development of new antibiotics for these pathogens is challenging because of the inability of most small mols. to accumulate inside GN bacteria. Using recently developed predictive guidelines for compound accumulation in Escherichia coli, we have converted the antibiotic Ribocil C, which targets the FMN (FMN) riboswitch, from a compound lacking whole-cell activity against wild-type GN pathogens into a compound that accumulates to a high level in E. coli, is effective against Gram-neg. clin. isolates, and has efficacy in mouse models of GN infections. This compound allows for the first assessment of the translational potential of FMN riboswitch binders against wild-type Gram-neg. bacteria.

Journal of the American Chemical Society published new progress about Acinetobacter baumannii. 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

Koskinen, Ari published the artcileNovel applications of the modified Polonovski reaction. III. Regiospecific functionalization of carbon atoms α to heterocyclic nitrogen, Recommanded Product: Methyl 1-methylpiperidine-2-carboxylate, the main research area is Polonovski reaction piperidine carboxylate; nitrile piperidine.

A nitrile substituent was introduced at the exocyclic α C atom of the piperidine N, making the center either nucleo- or electrophilic in subsequent transformations. Piperidineacetates I (R1 = Me, Et, Ph, R2 = R3 = H; R1 = R2 = Me, R3 = H; R1 = Me, R2 = H, R3 = Et, Δ3) and II (R4 = CO2Me) were oxidized and the product converted via a modified Polonovski reaction [(F3CCO)2O instead of Ac2O] to the cyano compounds III and II (R4 = cyano), as well as IV and V (R4 = cyano). The generality of the method, along with the ease of operation, high yields, and regiospecificity, make this reaction highly versatile for synthetic purposes.

Tetrahedron published new progress about Polonovski fragmentation. 1690-74-0 belongs to class piperidines, name is Methyl 1-methylpiperidine-2-carboxylate, and the molecular formula is C8H15NO2, Recommanded Product: Methyl 1-methylpiperidine-2-carboxylate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bu, Hong published the artcileDesign, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors, Product Details of C10H20N2O2, the main research area is eIF4E MNK inhibitor ETC 206; ETC-206; MNK1/2 kinases; MNKs inhibitor; eIF4E.

Mitogen-activated protein kinase (MAPK)-interacting kinases (MNKs) are located at the meeting-point of ERK and p38 MAPK signaling pathways, which can phosphorylate eukaryotic translation initiation factor 4E (eIF4E) at the conserved serine 209 exclusively. MNKs modulate the translation of mRNA involved in tumor-associated signaling pathways. Consequently, selective inhibitors of MNK1/2 could reduce the level of phosphorylated eIF4E. Series of imidazopyrazines, imidazopyridazines and imidazopyridines derivatives were synthesized and evaluated as MNK1/2 inhibitors. Several compounds exhibited great inhibitory activity against MNK1/2 and selected compounds showed moderate to excellent anti-proliferative potency against diffuse large B-cell lymphoma (DLBCL) cell lines. In particular, compound II-5 (MNK1 IC50 = 2.3 nM; MNK2 IC50 = 3.4 nM) exhibited excellent enzymic inhibitory potency and proved to be the most potent compound against TMD-8 and DOHH-2 cell lines with IC50 value of 0.3896μM and 0.4092μM resp. These results demonstrated that compound II-5 could be considered as a potential MNK1/2 inhibitor for further investigation.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 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

Wang, Xinran published the artcileDesign, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors, HPLC of Formula: 73874-95-0, the main research area is human liver microsome cell proliferation LSD1 inhibitor; 2-Aminopyrimidine; LSD1 inhibitors; Molecular docking; Structure-activity relationships.

AZD9291, with excellent pharmaceutical properties, has been reported to have certain LSD1 inhibitory activity. Therefore, we carried out structural optimization based on the AZD9291 skeleton to increase the LSD1 inhibitory potential of the compound Then, a series of 2-aminopyrimidine derivatives were designed and synthesized as LSD1 inhibitors, and their structure-activity relationships were studied. The most promising compound, X43, with an IC50 of 0.89 μM showed remarkable LSD1 selectivity not only to EGFRwt (>100-fold) but also to MAO-A/B (>50-fold). Further studies showed that X43 inhibited LSD1 activity and induced the apoptosis of A549 cells in a dose-dependent manner. Meanwhile, compound X43 showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, resp. Then, analyses of the stability of human liver microsomes, CYP inhibition and in vivo pharmacokinetics in rats showed that X43 had favorable profiles in vitro and in vivo and the potential for further study. Our findings suggested that a 2-aminopyrimidine-based LSD1 inhibitor deserves further investigation as a treatment for LSD1-overexpressing cancer.

Bioorganic Chemistry published new progress about Antiproliferative agents. 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

Yuan, Xinrui published the artcileDesign, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors, Quality Control of 73874-95-0, the main research area is pyridone aminal derivative preparation MNK1 MNK2 inhibitor colon cancer; MNK1/2; Pyridone–aminal; eFT508; eIF4E.

Excessive phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) plays a major role in the dysregulation of mRNA translation and the activation of tumor cell signaling. eIF4E is exclusively phosphorylated by mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2) on Ser209. So, MNK1/2 inhibitors could decrease the level of p-eIF4E and regulate tumor-associated signaling pathways. A series of pyridone-aminal derivatives were synthesized and evaluated as MNK1/2 inhibitors. Several compounds exhibited great inhibitory activity against MNK1/2 and selected compounds showed moderate to excellent anti-proliferative potency against hematol. cancer cell lines. In particular, compound 42i (MNK1 IC50 = 7.0 nM; MNK2 IC50 = 6.1 nM) proved to be the most potent compound against TMD-8 cell line with IC50 value of 0.91 μM. Furthermore, 42i could block the phosphorylation level of eIF4E in CT-26 cell line, and 42i inhibited the tumor growth of CT-26 allograft model significantly. These results indicated that compound 42i was a promising MNK1/2 inhibitor for the potent treatment of colon cancer.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Quality Control of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem