Month: November 2022

Shidore, Mahesh published the artcileBenzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer’s Agents: Synthesis and Biological Evaluation, HPLC of Formula: 39546-32-2, the publication is Journal of Medicinal Chemistry (2016), 59(12), 5823-5846, database is CAplus and MEDLINE.

A novel series of hybrid mols. were designed and synthesized by fusing the pharmacophoric features of cholinesterase inhibitor donepezil and diarylthiazole as potential multitarget-directed ligands for the treatment of Alzheimer’s disease (AD). The compounds showed significant in vitro anticholinesterase (anti-ChE) activity, the most potent compound I among them showing the highest activity (IC₅₀ value of 0.30 ± 0.01 μM) for AChE and (1.84 ± 0.03 μM) for BuChE. Compound I showed mixed inhibition of AChE in the enzyme kinetic studies. Some compounds exhibited moderate to high inhibition of AChE-induced Aβ_1-42 aggregation and noticeable in vitro antioxidant and antiapoptotic properties. Compound I showed significant in vivo anti-ChE and antioxidant activities. Furthermore, compound I demonstrated in vivo neuroprotection by decreasing Aβ_1-42-induced toxicity by attenuating abnormal levels of Aβ_1-42, p-Tau, cleaved caspase-3, and cleaved PARP proteins. Compound I exhibited good oral absorption and was well tolerated up to 2000 mg/kg, po, dose without showing toxic effects.

Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C8H8O3, HPLC of Formula: 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Tan, Yixuan published the artcileFacile construction of fluorescent C₇₀-COOH nanoparticles with advanced antibacterial and anti-biofilm photodynamic activity, HPLC of Formula: 826-36-8, the publication is Journal of Photochemistry and Photobiology, B: Biology (2022), 112507, database is CAplus and MEDLINE.

Photodynamic antibacterial therapy has been considered as one of the most promising treatments to alleviate the spread of multidrug resistant bacterial pathogens. Given the hypoxic environment of infectious tissues, photosensitizers with reduced oxygen-demand could exhibit superiority upon irradiation Herein reported is a novel C70-based photosensitizers synthesized by the facile one-step thiol-ene reaction. Various characterization techniques were employed to confirm the structural, photoluminescent properties, photostability and biocompatibility of the as-synthesized C70-COOH nanoparticles. Furthermore, they were capable of efficiently producing reactive oxygen species following both the type I and II mechanistic pathways, thus still generating adequate free radicals under hypoxic condition. Therefore, they could approach and destroy the bacterial cell membrane in the presence of visible light, thereby causing cytoplasmic leakage and eventually achieving broad-spectrum inactivation of four representative bacterial strains. Especially, methicillin-resistant Staphylococcus aureus (MRSA) were completely eliminated after merely 10 min irradiation, and the formation of its corresponding biofilm were also greatly inhibited by C70-COOH nanoparticles. These results provide new insights and opportunities for the development of hypoxia-tolerant fullerene-based photosensitizers to combat multidrug resistant bacterial and related infections.

Journal of Photochemistry and Photobiology, B: Biology published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C20H12N2O2, HPLC of Formula: 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Yang, Guang published the artcileType I macrophage activator photosensitizer against hypoxic tumors, Product Details of C9H17NO, the publication is Chemical Science (2021), 12(44), 14773-14780, database is CAplus and MEDLINE.

Photodynamic immunotherapy has emerged as a promising strategy to treat cancer. However, the hypoxic nature of most solid tumors and notoriously immunosuppressive tumor microenvironment could greatly compromise the efficacy of photodynamic immunotherapy. To address this challenge, we rationally synthesized a type I photosensitizer of TPA-DCR nanoparticles (NPs) with aggregation-enhanced reactive oxygen species generation via an oxygen-independent pathway. We demonstrated that the free radicals produced by TPA-DCR NPs could reprogram M0 and M2 macrophages into an anti-tumor state, which is not restricted by the hypoxic conditions. The activated M1 macrophages could further induce the immunogenic cell death of cancer cells by secreting pro-inflammatory cytokines and phagocytosis. In addition, in vivo anti-tumor experiments revealed that the TPA-DCR NPs could further trigger tumor immune response by re-educating tumor-associated macrophages toward M1 phenotype and promoting T cell infiltration. Overall, this work demonstrates the design of type I organic photosensitizers and mechanistic investigation of their superior anti-tumor efficacy. The results will benefit the exploration of advanced strategies to regulate the tumor microenvironment for effective photodynamic immunotherapy against hypoxic tumors.

Chemical Science published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C20H12N2O2, Product Details of C9H17NO.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

He, Suisui published the artcileSpatiotemporally controlled O₂ and singlet oxygen self-sufficient nanophotosensitizers enable the in vivo high-yield synthesis of drugs and efficient hypoxic tumor therapy, HPLC of Formula: 826-36-8, the publication is Chemical Science (2020), 11(33), 8817-8827, database is CAplus and MEDLINE.

Carrying out the in vivo syntheses of drugs toxic to tumors based on the specific features of the tumor microenvironment is critical for ensuring specific antitumor efficacy. However, achieving in situ high-yield synthetic toxic drugs from non-toxic agents and reducing their drug resistance in hypoxic tumors remain challenges. Herein we created a tumor-microenvironment-responsive porous Pt/Pt(IV) methylene blue coordination polymer nanoshuttle (Pt/PtMBCPNS) photosensitizer with spatiotemporally controlled O₂ and singlet oxygen (¹O₂) self-sufficient for the in vivo high-yield synthesis of drugs and efficient hypoxic tumor therapy. After being endocytosed, the nanophotosensitizer as a cascade catalyst was observed to effectively catalyze the conversion of endogenous H₂O₂ to O₂, and was hence found to play a dual role in the enhanced tumor therapy. PtMBCPNSs, upon being irradiated with red light, efficiently converted O₂ into ¹O₂. Subsequently, ¹O₂ oxidized non-toxic 1,5-dihydroxynaphthalene to form the anticancer agent juglone with a high yield. In addition, O₂ was found to be able to improve the hypoxic microenvironment without light irradiation, thus enhancing the antitumor efficacy of the produced drugs and reducing drug resistance. As a result, by enhancing the synergistic effect of the treatment, this nanophotosensitizer significantly inhibited the growth of tumors and avoided damage to normal tissues/organs. Collectively, this work highlights a robust nanoplatform with the spatiotemporally controlled in vivo high-yield synthesis of drugs and generation of O₂ to help overcome the current limitations of chem.-based therapies against hypoxic tumors.

Chemical Science published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, HPLC of Formula: 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wei, Ying published the artcileDegradation of enrofloxacin in aqueous by DBD plasma and UV: Degradation performance, mechanism and toxicity assessment, Formula: C9H17NO, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2022), 431(Part_3), 133360, database is CAplus.

Enrofloxacin (ENRO) as a highly toxic antibiotic poses great threats to human health and environmental safety. In this study, a novel technol. of coupling dielec. barrier discharge (DBD) and UV was investigated to efficiently degrade ENRO in aqueous, and had a higher degradation rate. The ENRO degradation rate achieved approx. 93.9% at 30 min, and approx. 1.20 g kWh-1 of energy yield (G50) was observed for the combined system. The addition of H₂O₂ and K₂S₂O₄ improved the ENRO degradation due to the generation of ·OH and ·SO₄^2-. In the presence of NO₃-, the ENRO degradation played a tendency to promote first and then decrease, and the presence of SO₄^2-resulted in the pos. effect, while the neg. effect was shown in the presence of Cl^– and CO₃^2-. The trapping experiment indicated that ·OH played an important part in the ENRO degradation The addition of UV into the DBD system decreased H₂O₂ concentration in deionized water, and increased ·OH concentration The DFT anal. showed the degradation mechanisms of ENRO at a mol. level. The degradation of ENRO mainly involved the oxidation of the piperazine group, the removal of Et acetate and the substitution of the F atom. The toxicity of ENRO and its degradation intermediates was evaluated.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C40H35N7O8, Formula: C9H17NO.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Su, Yiping published the artcileIn situ synthesis of Tree-branch-like Copper-manganese oxides nanoarrays supported on copper foam as a superior efficiency Fenton-like catalyst for enhanced degradation of 4-chlorophenol, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Applied Surface Science (2022), 153241, database is CAplus.

Recently, considerable attention has been paid to develop novel Fenton-like oxidation systems for environmental remediation. The activation of periodate (NaIO₄) is a desirable oxidation process that drive redox reactions to produce abundant reactive oxygen species (ROS) by a suitable activator. This study reports a simple hydrothermal-calcination route for forming novel tree-branch-like copper-manganese oxides (CuMnOx@MnOx, CMM) nanoarrays, and the production of radical species from NaIO₄ induced by CMM for the removal of rhodamine B and 4-chlorophenol from wastewater. The synergistic effects of Cu oxides and Mn oxides composite significantly elevated the activation of periodate, exhibited excellent degradation performance in the CMM/NaIO₄. Furthermore, reduced copper species and mixed-valence manganese species play a major role in reaction via XPS anal. Addnl., the underlying degradation mechanism of this work was systematically researched by radical quenching tests and EPR anal. Superoxide anion radical (·O^–2) was the major free radicals in this system, simultaneously the production of non-radical singlet oxygen (¹O₂) via the electron transfer, which are contributed to remove organic pollutants. This work provides a facile way for fabricating monolithic multi-component metal oxides, and new insights into understand activation mechanism of manganese-based periodate activator.

Applied Surface Science published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C3H3Br2ClO, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Zhao, Xuna published the artcileIn Situ Generated TEMPO Oxoammonium Salt Mediated Tandem Cyclization of β-Oxoamides with Amine Hydrochlorides for the Synthesis of Pyrrolin-4-ones, Computed Properties of 219543-09-6, the publication is Journal of Organic Chemistry (2017), 82(12), 6125-6132, database is CAplus and MEDLINE.

In the presence of TEMPO (via its in situ-generated oxoammonium salt), acetoacetamides MeCOCH₂CONHR (R = Ph, 4-MeOC₆H₄, 3-MeOC₆H₄, 2-MeOC₆H₄, 4-MeC₆H₄, 2-MeC₆H₄, 2,4-Me₂C₆H₃, 4-ClC₆H₄, 3-ClC₆H₄, 2-ClC₆H₄, 4-EtO₂CC₆H₄, PhCH₂, t-Bu) underwent chemoselective oxidative cyclocondensations with amine hydrochlorides R¹NH₂·HCl (R¹ = Ph, 4-MeOC₆H₄, 4-MeC₆H₄, 3-MeC₆H₄, 2-MeC₆H₄, 4-ClC₆H₄, 3-ClC₆H₄, HCCCH₂, PhCH₂, n-Pr, H) or ammonium chloride in DMF to yield oxopyrroledicarboxamides I (R = Ph, 4-MeOC₆H₄, 3-MeOC₆H₄, 2-MeOC₆H₄, 4-MeC₆H₄, 2-MeC₆H₄, 2,4-Me₂C₆H₃, 4-ClC₆H₄, 3-ClC₆H₄, 2-ClC₆H₄, 4-EtO₂CC₆H₄, PhCH₂, t-Bu; R¹ = Ph, 4-MeOC₆H₄, 4-MeC₆H₄, 3-MeC₆H₄, 2-MeC₆H₄, 4-ClC₆H₄, 3-ClC₆H₄, HCCCH₂, PhCH₂, n-Pr, H) in 48-82% yields. Detailed mechanistic studies disclosed that TEMPO oxoammonium salt generated in situ was crucial for the transformation involving the formation of enaminone precursors in situ by condensation of the β-oxoamides with amines, followed by sequential oxidative coupling with β-oxoamides, intramol. cyclization, and 1,2-alkyl migration steps.

Journal of Organic Chemistry published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C7H10O4, Computed Properties of 219543-09-6.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Guo, Shuai published the artcileUnveiling the mechanism of NO_x precursor formation during sewage sludge pyrolysis: Effects of carbohydrate-protein interactions, Synthetic Route of 826-36-8, the publication is Journal of Environmental Chemical Engineering (2022), 10(3), 107579, database is CAplus.

Municipal sewage sludge poses environmental and health risks, and thus, requires proper disposal using pyrolytic techniques. However, these techniques are hindered by the production of NH3 and HCN (NO_x precursors) by the sludge. Hence, a comprehensive understanding of NH³ and HCN formation during sludge pyrolysis is required to minimize its NOx footprint. As sludge N mainly occurs in proteins forms, its transformations can be modeled using amino acids. Here, we aimed to the study the mechanism by which carbohydrates influence the formation of NO_x precursors during sludge protein pyrolysis at different temperatures using glutamic acid, tyrosine, and histidine as protein models and cellulose and lignin as carbohydrate models. During pyrolysis, the release of NH³ and HCN was promoted by high temperatures and inhibited by carbohydrates. Despite this inhibitory effect, the results suggested that the release of NH3 should be considered for samples rich in aliphatic amino acids. For glutamic acid and tyrosine, NOx precursor formation was inhibited by N fixation in coke under the action of volatiles produced during carbohydrate pyrolysis. For glutamic acid, adding cellulose and lignin increased the coke-N content by 25.32% and 44.73% at 700°C. For histidine, this effect was ascribed to the ring-opening reactions induced by the free radical products of carbohydrate decomposition and the enhanced transfer of N-containing compounds to tar after ring-opening recombination. Further, heterocyclic-N within tar increased to 69.12% due to lignin-histidine interactions at 700°C. The results of this study can assist in regulating sludge protein pyrolysis intended for minimizing the production of NO_x precursors.

Journal of Environmental Chemical Engineering published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Synthetic Route of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Mei, Haibo published the artcileA Selectfluor-promoted oxidative reaction of disulfides and amines: access to sulfinamides, Category: piperidines, the publication is Organic & Biomolecular Chemistry (2020), 18(19), 3761-3766, database is CAplus and MEDLINE.

An unprecedented transition-metal-free oxidative reaction of disulfides and amines with Selectfluor as a mild oxidant under aerobic conditions was developed. This reaction was conducted under mild conditions and tolerated a wide range of coupling partners including disulfides and amines, affording the corresponding sulfinamide products in good chem. yields. Furthermore, this reaction could be used in gram-scale synthesis. This reaction enriches the research content of Selectfluor and provides a valuable vista for the convenient synthesis of sulfinamides.

Organic & Biomolecular Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Sun, Ping published the artcileStrategic combination of N-doped graphene and g-C₃N₄: Efficient catalytic peroxymonosulfate-based oxidation of organic pollutants by non-radical-dominated processes, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Applied Catalysis, B: Environmental (2020), 119005, database is CAplus.

two metal-free materials, N-doped graphene (rGO-N) and g-C₃N₄, were strategically combined to prepare a novel g-C₃N₄/rGO-N composite to activate peroxymonosulfate (PMS). this g-C₃N₄/rGO-N composite had a large sp. surface area and high graphite-rich N content; thus, exhibited excellent catalytic performance due to the synergistic effect of g-C₃N₄ and rGO-N. the oxidative system effectively degraded various pollutants (acid orange 7, orange G, ciprofloxacin, bisphenol A). radical quenching experiments and ESR spectra anal. showed the novel carbonaceous composite could provide PMS-based, non-radical oxidative pollutant degradation unlike previously reported catalysts for observed degradation via a radical-dominated pathway. real-time wastewater treatment experiments demonstrated the oxidative system potential for environmental remediation applications. the combination strategy provided an innovative approach to fabricate binary metal-free carbonaceous catalysts to perform PMS-based, non-radical oxidative pollutant degradation

Applied Catalysis, B: Environmental published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C47H82N4O15, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem