Month: December 2022

Dileep, K. V. published the artcilePiperidine-4-carboxamide as a new scaffold for designing secretory glutaminyl cyclase inhibitors, Application In Synthesis of 39546-32-2, the publication is International Journal of Biological Macromolecules (2021), 415-423, database is CAplus and MEDLINE.

Alzheimer’s disease (AD), a common chronic neurodegenerative disease, has become a major public health concern. Despite years of research, therapeutics for AD are limited. Overexpression of secretory glutaminyl cyclase (sQC) in AD brain leads to the formation of a highly neurotoxic pyroglutamate variant of amyloid beta, pGlu-Aβ, which acts as a potential seed for the aggregation of full length Aβ. Preventing the formation of pGlu-Aβ through inhibition of sQC has become an attractive disease-modifying therapy in AD. In this current study, through a pharmacophore assisted high throughput virtual screening, we report a novel sQC inhibitor (Cpd-41) with a piperidine-4-carboxamide moiety (IC₅₀ = 34μM). Systematic mol. docking, MD simulations and X-ray crystallog. anal. provided atomistic details of the binding of Cpd-41 in the active site of sQC. The unique mode of binding and moderate toxicity of Cpd-41 make this mol. an attractive candidate for designing high affinity sQC inhibitors.

International Journal of Biological Macromolecules 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 C6H12N2O, Application In Synthesis of 39546-32-2.

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

Wan, Wen-jing published the artcileImprovement of 2,2,6,6-tetramethyl-4-piperidinamine synthesis via catalytic amination, Product Details of C9H17NO, the publication is Gaoxiao Huaxue Gongcheng Xuebao (2020), 34(2), 457-462, database is CAplus.

2,2,6,6-Tetramethylpiperidinamine as light stabilizer of hindered amines was synthesized via catalytic amination of 2,2,6,6-tetramethylpiperidone. Imine formation was promoted by adjusting reaction system pH, which facilitated the catalytic amination under mild condition. The selectivity of the product was increased. When studied under pH∼12.5, reaction temperature 60°C and pressure 2 MPa, the selectivity of TEMP was up to 95.2%. The result shows that pH=12.5 is the most favorable condition for the formation of TEMP.

Gaoxiao Huaxue Gongcheng Xuebao 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 C20H18BrN3, Product Details of C9H17NO.

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

Carocci, Alessia published the artcileSynthesis and Evaluation of Voltage-Gated Sodium Channel Blocking Pyrroline Derivatives Endowed with Both Antiarrhythmic and Antioxidant Activities, Formula: C9H17NO, the publication is ChemMedChem (2021), 16(3), 578-588, database is CAplus and MEDLINE.

Under the hypothesis that cardioprotective agents might benefit from synergism between antiarrhythmic activity and antioxidant properties, a small series of mexiletine analogs were coupled with the 2,2,5,5-tetramethylpyrroline moiety, known for its antioxidant effect, in order to obtain dual-acting drugs potentially useful in the protection of the heart against post-ischemic reperfusion injury. The pyrroline derivatives reported herein were found to be more potent as antiarrhythmic agents than mexiletine and displayed antioxidant activity. The most interesting tetramethylpyrroline congener, a tert-butyl-substituted analog, was at least 100 times more active as an antiarrhythmic than mexiletine.

ChemMedChem 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, Formula: C9H17NO.

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

Frawley, Thomas F. published the artcileAdrenal cortical function during isoniazid therapy for pulmonary tuberculosis, Application of 1-Ethylpiperidin-3-ol, the publication is American Review of Tuberculosis (1954), 841-51, database is CAplus.

The nature of the host’s response during isoniazid therapy for pulmonary tuberculosis suggested a possible adrenal cortical influence. By utilizing eosinophil levels, 17-keto steroid, uric acid, creatinine, and 17-hydroxy corticoid excretion patterns, the level of adrenal activity was determined before and during isoniazid therapy. Adrenal cortical responsiveness was assessed by the 8-hr. intravenous corticotropin test both before and during therapy. In no instance in either the resting or stimulated state was a significant or consistent deviation from the normal observed. A gradual rise in circulating eosinophils occurred during isoniazid therapy. The urinary uric acid-creatinine ratio varied directly with the disease progress and further use of this as an index of degree of disease activity is suggested.

American Review of Tuberculosis published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Application of 1-Ethylpiperidin-3-ol.

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

Knutson, Daniel E. published the artcileImproved scale-up synthesis and purification of clinical asthma candidate MIDD0301, Formula: C19H21N, the publication is Organic Process Research & Development (2020), 24(8), 1467-1476, database is CAplus and MEDLINE.

An improved and scalable synthesis of MIDD0301, a pos. GABAA receptor modulator that is under development as oral and inhaled treatments for asthma was reported. The starting material to generate MIDD0301 is 2-amino-5-bromo-2′-fluorobenzophenone, which has a non-basic nitrogen due to electron withdrawing substituents in ortho and para positions, reducing its reactivity towards activated carboxylic acids. Investigations of peptide coupling reagents on multigram scale resulted in moderate yields due to incomplete conversions. Secondly, basic conditions used for the formation of the seven-member 1,4-diazepine ring resulted in racemization of the chiral center. It was found that neutral conditions comparable to the pKa of the primary amine where sufficient to support the formation of the intramol. imine but did not enable the simultaneous removal of the protecting group. Both difficulties were overcome with the application of the N-carboxyanhydride of D-alanine. Activated in the presence of acid, this compound reacted with non-basic 2-amino-5-bromo-2′-fluorobenzophenone and formed the 1,4-diazepine upon neutralization with triethylamine. Carefully designed workup procedures and divergent solubility of the synthesis intermediates in solvents and solvent combinations were utilized to eliminate the need for column chromatog. To improve compatibility with large scale reactors, temperature-controlled slow addition of reagents generated the imidazodiazepine at -20°C. All intermediates were isolated with a purity of >97% and impurities were identified and quantified. After the final hydrolysis step, MIDD0301 was isolated with a 44% overall yield and purity of 98.9% after recrystallization The enantiomeric excess was higher than 99.0%.

Organic Process Research & Development published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C19H21N, Formula: C19H21N.

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

Ren, Zhongfei published the artcileIbuprofen degradation using a Co-doped carbon matrix derived from peat as a peroxymonosulphate activator, HPLC of Formula: 826-36-8, the publication is Environmental Research (2021), 110564, database is CAplus and MEDLINE.

The wider presence of pharmaceuticals and personal care products in nature is a major cause for concern in society. Among pharmaceuticals, the anti-inflammatory drug ibuprofen has commonly been found in aquatic and soil environments. We produced a Co-doped carbon matrix (Co-P 850) through the carbonization of Co²⁺ saturated peat and used it as a peroxymonosulfate activator to aid ibuprofen degradation The properties of Co-P 850 were analyzed using field emission SEM, energy filtered transmission electron microscopy and XPS. The characterization results showed that Co/Fe oxides were generated and tightly embedded into the carbon matrix after carbonization. The degradation results indicated that high temperature and slightly acidic to neutral conditions (pH = 5 to 7.5) promoted ibuprofen degradation efficiency in the Co-P 850/peroxymonosulfate system. Anal. showed that approx. 52% and 75% of the dissolved organic carbon was removed after 2 h and 5 h of reaction time, resp. Furthermore, the existence of chloride and bicarbonate had adverse effects on the degradation of ibuprofen. Quenching experiments and ESR anal. confirmed that SO·-4, ·OH and O ·^-2 radicals together contributed to the high ibuprofen degradation efficiency. In addition, we identified 13 degradation intermediate compounds and an ibuprofen degradation pathway by mass spectrometry anal. and quantum computing. Based on the results and methods presented in this study, we propose a novel way for the synthesis of a Co-doped catalyst from spent NaOH-treated peat and the efficient catalytic degradation of ibuprofen from contaminated water.

Environmental Research 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

Beuchel, Andreas published the artcileStructure-Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors, COA of Formula: C6H12N2O, the publication is ACS Medicinal Chemistry Letters (2022), 13(3), 417-427, database is CAplus and MEDLINE.

Mycobacterium abscessus causes difficult-to-cure pulmonary infections. The bacterium is resistant to most anti-infective agents, including first line antituberculosis (anti-TB) drugs. MMV688844 (844) is a piperidine-4-carboxamide (P4C) with bactericidal properties against M. abscessus. We recently identified DNA gyrase as the mol. target of 844. Here, we present in silico docking and genetic evidence suggesting that P4Cs display a similar binding mode to DNA gyrase as gepotidacin. Gepotidacin is a member of the Novel Bacterial Topoisomerase Inhibitors (NBTIs), a new class of nonfluoroquinolone DNA gyrase poisons. Thus, our work suggests that P4Cs present a novel structural subclass of NBTI. We describe structure-activity relationship studies of 844 leading to analogs showing increased antibacterial activity. Selected derivatives were tested for their inhibitory activity against recombinant M. abscessus DNA gyrase. Further optimization of the lead structures led to improved stability in mouse plasma and increased oral bioavailability.

ACS Medicinal Chemistry Letters 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 C6H12N2O, COA of Formula: C6H12N2O.

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

Reynaud, Pierre published the artcileO-Dialkylaminoalkyl thioesters, analogs of adiphenine and related esters, Recommanded Product: 1-Ethylpiperidin-3-ol, the publication is European Journal of Medicinal Chemistry (1975), 10(3), 262-7, database is CAplus.

Imidates RCR1R2C(:NH)OEt [R = Ph, Pr; R1 = Ph, cyclopentyl, Pr; R2 = H; R1R2 = (CH2)4] reacted with H2S to give RCR1R2C(S)OEt; and transesterification of the latter yields eight resp. RCR1R2C(S)OR3 [R3 = CH2CH2NEt2, CH2CH2NMe2, 2-(1-piperidinyl)ethyl, 1-ethyl-3-piperidinyl], which demonstrated spasmolytic activity and were effective against induced tremor.

European Journal of Medicinal Chemistry published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Recommanded Product: 1-Ethylpiperidin-3-ol.

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

Dong, Xiongbo published the artcileDiatomite supported hierarchical 2D CoNi₃O₄ nanoribbons as highly efficient peroxymonosulfate catalyst for atrazine degradation, SDS of cas: 826-36-8, the publication is Applied Catalysis, B: Environmental (2020), 118971, database is CAplus.

Reactive oxygen radicals generated by peroxymonosulfate (PMS) activation exhibit great potential to treat refractory pollutants of emerging concern; however, mass production of efficient, cost-effective catalysts for PMS activation is a long-term goal for its widespread practical application. A CoNi₃O₄/diatomite hybrid was prepared via vertically oriented growth of two dimensional (2D) CoNi₃O₄ nanoribbons of at. layer-thickness on a cost-effective diatomite template. Distinct from stacked CoNi₃O₄, the CoNi₃O₄/diatomite composite has abundant exposed edges, sharp corners, and open diffusion channels. Abundant exposed edges and sharp corners create more open space and active sites for PMS activation. Open diffusion channels accelerate PMS and pollutants migration. Such properties provide CoNi₃O₄/diatomite hybrid excellent PMS activation efficiency. Sulfate radical played the dominant role in atrazine degradation, and superoxide radical contributed to reversible redox cycle of Co²⁺/Co³⁺ and Ni²⁺/Ni³⁺. This work provided a strategy for cost-effective mass production of Fenton-like 2D catalysts.

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 C9H17NO, SDS of cas: 826-36-8.

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

del Pozo, Cristina published the artcileConverting coffee silverskin to value-added products by a slow pyrolysis-based biorefinery process, Name: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Fuel Processing Technology (2021), 106708, database is CAplus.

This work aims to transform coffee silverskin (CSS), the only waste from the coffee roasting process, that worldwide amounts to about 76 million kg/yr, into value-added products within an integrated slow pyrolysis process. The study, performed at 280°C, 400°C and 500°C, determined the potential applications of the resulting fractions. Biochar has been studied as an adsorbent of organic pollutants in water, using methylene blue (MB) and methyl orange (MO), which are resp. cationic and anionic aromatic dyes, as model compounds, and with 400°C biochar giving the highest removal values, at 98% with MB and 40% with MO. Moreover, CSS biochar could be used to obtain renewable energy from its combustion, with 22.6-24.2 MJ/kg calorific values. The liquid fraction could be a potential source of caffeine, among phenolics, with 400°C aqueous phase presenting the highest concentration of caffeine (14.3 g/L). Concerning the gas fraction, it could be used to obtain heat for biomass drying before pyrolysis. Hence, use of the pyrolysis products as described would allow zero-waste to be achieved in the coffee roasting industry, thus promoting the green and circular economy and production of green chems. and materials in a biorefinery context.

Fuel Processing Technology 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, Name: 2,2,6,6-Tetramethylpiperidin-4-one.

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