Category: amides-buliding-blocks

Yang, Long published the artcileElectrochemical B-H Nitrogenation: Access to Amino Acid and BODIPY-Labeled nido-Carboranes, Name: N,N-Diethylisonicotinamide, the publication is Angewandte Chemie, International Edition (2021), 60(3), 1482-1487, database is CAplus and MEDLINE.

Electrocatalyzed oxidative B-H nitrogenations of nido-carborane (nido-7,8-C₂B₉H₁₂^–) with N-heterocycles have been established, enabling the preparation of various N-substituted nido-carboranes without chem. oxidants or metal catalyst under ambient conditions. The electrolysis manifold occurred with high levels of efficiency as well as chemo- and position- selectivity, employing sustainable electricity as the sole oxidant. The strategy set the stage for a user-friendly access to novel amino acid and fluorogenic boron-dipyrrin (BODIPY)-labeled nido-carborane hybrids.

Angewandte Chemie, International Edition published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C9H5ClO4S, Name: N,N-Diethylisonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nillert, Nutchareeporn published the artcileClausena Harmandiana root extract attenuated cognitive impairments via reducing amyloid accumulation and neuroinflammation in Aβ_1-42-induced rats, HPLC of Formula: 169590-42-5, the publication is BMC Complementary Medicine and Therapies (2022), 22(1), 108, database is CAplus and MEDLINE.

Alzheimer’s disease (AD) pathogenesis is associated with amyloid-β (Aβ)-induced neuroinflammation. In AD, the activation of microglia caused by Aβ accumulation is followed by the synthesis and release of pro-inflammatory cytokines, including interleukin-1β (IL-1β) and tumor necrosis factor-α (TNFα), and ultimately leads to cognitive impairments. Clausena harmandiana (CH) is a medicinal plant in the Rutaceae family and has been used in folk medicine to relieve illnesses such as stomachache and headache, and as a health tonic. Interestingly, CH root extract (CHRE) has several anti-inflammatory and other pharmacol. activities, but there are no studies in AD-like animal models. This study aims to evaluate the effects of CHRE on cognitive impairments, increased Aβ1-42 protein levels, and neuroinflammation in Aβ1-42-induced rats. Forty-eight adult male Sprague-Dawley rats (250-300 g) were randomly divided into 6 groups (n = 8) of the sham control, V + Aβ, CB + Aβ CHRE125 + Aβ, CHRE250 + Aβ, and CHRE500 + Aβ. Sodium CM-cellulose, Celebrex (10 mg/kg BW) and CHRE (125, 250, and 500 mg/kg BW) were given orally or without any treatment for 35 days. On day 21, aggregated Aβ1-42 at a concentration of 1μg/μl were injected into both lateral ventricles (1μl/side) of all treated rats, while sterilized normal saline were injected to untreated rats. Ten days later, the novel object recognition test was performed to assess their recognition memory. At the end of the test period, an overdose of thiopental sodium (120 mg/kg BW) and transcardial perfusion with 0.9% normal saline solution were used to euthanize all rats. Then Aβ1-42 protein levels and the expression of inflammatory markers (CD11b-pos. microglia, IL-1β, and TNFα) were investigated in the cerebral cortex and hippocampus. Pretreatment with CHRE at all doses could attenuate short- and long-term impairments in recognition memory. Addnl., CHRE also inhibited the increase of Aβ1-42 protein levels and the expression of inflammatory markers in both brain regions as well as receiving Celebrex. This suggests that preventive treatment of CHRE might be a potential therapy against cognitive impairments via reducing Aβ1-42 protein levels and neuroinflammation caused by Aβ1-42.

BMC Complementary Medicine and Therapies published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Puzari, Amlan published the artcileBinuclear Pd(II) complexes with multidentate Schiff base ligands: synthesis, catalysis, and antibacterial properties, Synthetic Route of 1453-82-3, the publication is Monatshefte fuer Chemie (2022), 153(5-6), 435-442, database is CAplus.

Abstract: Three new binuclear palladium(II) complexes with multidentate Schiff base ligands were synthesized and characterized by FTIR, UV-visible, ¹H-NMR, ESI-MS, and CHN anal. The complexes were successfully applied as catalysts for hydration of nitriles to amides. Using one of the complexes, a wide range of aryl/heteroaryl nitriles were efficiently converted to corresponding amides in moderate-to-excellent yields with low catalyst loading (0.8 mol%). In addition, the complexes were also tested for antibacterial activity against two gram-pos. and two gram-neg. bacteria using Kirby Bauer’s disk diffusion method. However, to the authors’ surprise, among the three complexes, only one complex showed growth inhibitory effect against gram-pos. bacteria, Bacillus subtilis, for which min. inhibitory concentration (MIC) is 30μg cm^-3.

Monatshefte fuer Chemie published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Synthetic Route of 1453-82-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rahman, Taskia published the artcileActivated Mont K10-Carbon supported Fe₂O₃: A versatile catalyst for hydration of nitriles to amides and reduction of nitro compounds to amines in aqueous media, Application In Synthesis of 1453-82-3, the publication is Journal of Chemical Sciences (Berlin, Germany) (2021), 133(1), 27, database is CAplus.

The iron oxide was successfully supported on activated clay/carbon through an exptl. viable protocol for both hydration of nitriles RCN (R = Ph, pyridin-4-yl, 4-bromophenyl, etc.) to RC(O)NH₂ to amides and reduction of nitro compounds R¹NO₂ (R¹ = Ph, 3-nitrophenyl, 2-trifluoromethyl-4-nitrophenyl, etc.) to amines R¹NH₂. The as-prepared catalyst has been extensively characterized by XPS, SEM-EDX, TEM, TGA, BET surface area measurements and powd. X-ray diffraction (PXRD). A wide variety of substrates could be converted to the desired products with good to excellent yields by using water as a green solvent for both the reactions. The catalyst was recyclable and reusable up to six consecutive cycles without compromising its catalytic proficiency.

Journal of Chemical Sciences (Berlin, Germany) published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Application In Synthesis of 1453-82-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hwang, Jimin published the artcileMulticomponent Petasis Reaction for the Synthesis of Functionalized 2-Aminothiophenes and Thienodiazepines, Name: 2-Cyano-N-ethylacetamide, the publication is ACS Combinatorial Science (2020), 22(10), 495-499, database is CAplus and MEDLINE.

Multicomponent Petasis reaction has been widely applied for the synthesis of functionalized amine building blocks and biol. active compounds Employing primary aromatic amines that are not typical reactive substrates contributes to expand the application scope of the Petasis reaction. In this study, we demonstrated the synthesis of functionalized 2-aminothiophenes using Gewald-reaction-derived 2-aminothiophenes as the amine substrates, whose low reactivity in the Petasis reaction was overcome using hexafluoro-2-propanol as the solvent in a mild condition. The obtained Petasis products are amenable for further transformations owing to the presence of multiple functional handles. A following intramol. cyclization of selected Petasis products afforded substituted tricyclic heterocycles that incorporate a pharmaceutically interesting thienodiazepine moiety.

ACS Combinatorial Science published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Name: 2-Cyano-N-ethylacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Leitão, Andrea Whitehurst Ary published the artcileCelecoxib in the treatment of orofacial pain and discomfort in rats subjected to a dental occlusal interference model., SDS of cas: 169590-42-5, the publication is Acta cirurgica brasileira (2022), 37(5), e370506, database is MEDLINE.

PURPOSE: To evaluate the effect of a selective cyclooxygenase 2 (COX-2) inhibitor on trigeminal ganglion changes and orofacial discomfort/nociception in rats submitted to an experimental model of dental occlusal interference (DOI). METHODS: Female Wistar rats (180-200 g) were divided into five groups: a sham group (without DOI) (n=15); and four experimental groups with DOI treated daily with 0.1 mL/kg saline (DOI+SAL), 8, 16, or 32 mg/kg celecoxib (DOI+cel -8, -16, -32) (n=30/group). The animals were euthanized after one, three, and seven days. The bilateral trigeminal ganglia were analyzed histomorphometrically (neuron cell body area) and immunohistochemically (COX-2, nuclear factor-kappa B [NFkB], and peroxisome proliferator-activated receptor-y [PPARy]). A bilateral nociception assay of the masseter muscle was performed. The number of bites/scratches, weight, and grimace scale scores were determined daily. One-way/two-way analysis of variance (ANOVA)/Bonferroni post hoc tests were used (P < .05, GraphPad Prism 5.0). RESULTS: DOI+SAL showed a reduction in neuron cell body area bilaterally, whereas DOI+cel-32 exhibited a significative increase in neuron cell body area compared with DOI+SAL group (P < 0.05). The ipsilateral (P=0.007 and P=0.039) and contralateral (P < 0.001 and P=0.005) overexpression of COX-2 and NFkB and downregulation of PPARy (P=0.016 and P < 0.001) occurred in DOI+SAL, but DOI+cel-32 reverted this alteration. DOI+SAL showed increase in isplateral (P < 0.001) and contralateral (P < 0.001) nociception, an increased number of bites (P=0.010), scratches (P < 0.001), and grimace scores (P=0.032). In the group of DOI+cel-32, these parameters were reduced. CONCLUSIONS: Celecoxib attenuated DOI-induced transitory nociception/orofacial discomfort resulting from trigeminal COX-2 overexpression.

Acta cirurgica brasileira published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, SDS of cas: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Brulet, Jeffrey W. published the artcileLiganding Functional Tyrosine Sites on Proteins Using Sulfur-Triazole Exchange Chemistry, Name: Isonicotinamide, the publication is Journal of the American Chemical Society (2020), 142(18), 8270-8280, database is CAplus and MEDLINE.

Tuning reactivity of sulfur electrophiles is key for advancing click chem. and chem. probe discovery. To date, activation of the sulfur electrophile for protein modification has been ascribed principally to stabilization of a fluoride leaving group (LG) in covalent reactions of sulfonyl fluorides and arylfluorosulfates. We recently introduced sulfur-triazole exchange (SuTEx) chem. to demonstrate the triazole as an effective LG for activating nucleophilic substitution reactions on tyrosine sites of proteins. Here, we probed tunability of SuTEx for fragment-based ligand discovery by modifying the adduct group (AG) and LG with functional groups of differing electron-donating and -withdrawing properties. We discovered the sulfur electrophile is highly sensitive to the position of modification (AG vs. LG), which enabled both coarse and fine adjustments in solution and proteome activity. We applied these reactivity principles to identify a large fraction of tyrosine sites (~30%) on proteins (~44%) that can be liganded across >1500 probe-modified sites quantified by chem. proteomics. Our proteomic studies identified noncatalytic tyrosine and phosphotyrosine sites that can be liganded by SuTEx fragments with site specificity in lysates and live cells to disrupt protein function. Collectively, we describe SuTEx as a versatile covalent chem. with broad applications for chem. proteomics and protein ligand discovery.

Journal of the American Chemical Society published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Name: Isonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Moral, Alberto published the artcileDevelopment of sol-gel silica-based mixed-mode zwitterionic sorbents for determining drugs in environmental water samples, Synthetic Route of 137862-53-4, the publication is Journal of Chromatography A (2022), 463237, database is CAplus and MEDLINE.

Four novel mixed-mode zwitterionic silica-based functionalized with strong moieties sorbents were synthesized and evaluated through solid-phase extraction (SPE) to determine acidic and basic drugs in environmental water samples. All sorbents had the same functionalization: quaternary amine and sulfonic groups and C18 chains so that hydrophobic and strong cationic exchange (SCX) and strong anionic exchange (SAX) interactions could be exploited, in addition, two of them had carbon microparticles embedded. All sorbents retained both acidic and basic compounds in the preliminary assays but only the basic compounds were retained selectively through ionic exchange interactions when a clean-up step was introduced. The SPE method was therefore optimized to promote the selective retention of the basic compounds, initially with the two best-performing sorbents. After optimization of the SPE protocol, these sorbents were evaluated for the anal. of environmental water samples using liquid chromatog.-tandem mass spectrometry (LC-MS/MS). The method with the best-performing sorbent was then validated with 100 mL of river samples and 50 mL of effluent wastewater samples in terms of apparent recoveries (%Rapp) spiking samples at 50 ng/L (river) and 200 ng/L (river and effluent), matrix effect, linear range, method quantification and detection limits, repeatability, and reproducibility. It should be highlighted that %Rapp ranged from 40 to 85% and matrix effects ranged from -17 to -4% for spiked river samples. When the method was applied to river and effluent wastewater samples, most compounds were found in the range from 24 to 1233 ng/L with detection limits from 1 to 5 ng/L.

Journal of Chromatography A published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Synthetic Route of 137862-53-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Canonica, Luigi published the artcileSynthetic analeptics. I. Hydroxybenzoic acid diethylamides, Category: amides-buliding-blocks, the publication is Annali di Chimica (Rome, Italy) (1955), 205-15, database is CAplus.

Of the dialkylamides studied, the best analeptic activity was present in the diethylamides of vanillic acid. Analogs prepared and studied for pharmacol activity were the following benzoic acid diethylamides (substituent given): 4-acetoxy, m. 80-1°; 3-methoxy, b_1.7 132-4°; 2-hydroxy-4-methoxy, m. 121-2°; 2,4-dimethoxy; 2-hydroxy-5-methoxy, m. 103-4°; 3-chloro-4-hydroxy (I); 3-bromo-4-hydroxy (II), m. 158-9°; 3-nitro-4-hydroxy, m. 123-4° (decomposition); 3-chloro-4-acetoxy, m. 89° (crystallized from dilute MeOH); 3-hydroxy, m. 83°; 2-acetoxy, b₁₀ 178-80°; 2-hyhydroxy, m. 104-5°; 3-methoxy-4-hydroxy (III); 3-methoxy-4-acetoxy (IV); 3-ethoxy-4-hydroxy (V), m. 92-3°; 3-ethoxy-4-acetoxy (VI); 4-hydroxy, m. 121.5°; 4-methoxy, m. 42°; 2-acetoxy-4-methoxy, m. 120-1°; 3-bromo-4-acetoxy, m. 94-5° (crystallized from C₆H₆-petr. ether); 3,4,5-trimethoxy, m. 54°, b₅ 203-4°. Piperonylic acid diethylamide, m. 64-5° (from H₂O), and isonicotinic acid diethylamide, b₁₅ 162-4°, were also prepared In general, the acids were converted to acid chlorides with PCl₅ in CS₂ and then to the diethylamide with Et₂NH in C₆H₆. Analeptic activity is given relative to cyclopentamethylenetetrazole. Most active compounds were I to VI in decreasing consecutive order. The presence of a single OH group or OAc increased activity but not significantly. Compounds with a 3-OR group where R = Me or Et were highly active.

Annali di Chimica (Rome, Italy) published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Merzoug, Amina published the artcileMolecular docking study of the acetylcholinesterase inhibition, Category: amides-buliding-blocks, the publication is Current Issues in Pharmacy and Medical Sciences (2021), 34(1), 20-27, database is CAplus.

While Alzheimer disease is the most common form of dementia, acetylcholinesterase is an interesting therapeutic target for the development of new anti-Alzheimer’s disease drugs. In order to discover potential compounds inhibiting this protein target, a mol. docking study of a similar collection of 1-[[2,4-bis[(E)hydroxyiminomethyl] pyridin-1-ium-1-yl]methoxymethyl] pyridin-1-ium-4-carboxamide (HLO) inhibitor from ZINC database using FlexX program was realized. Before performing the mol. docking, FlexX was validated by Root mean square deviation test to determine the reproducibility of the docking program. The strategy undertaken in this study permitted us to propose products 4-[[2-[(Z)-N’-hydroxycarbamimidoyl]-4-pyridyl]methylamino] benzamide and N-[(E)-[1-(4-nitrophenyl)pyrrol-2-yl]methylene amino]isonicotinamide as potential new inhibitors of humane acetylcholinesterase. The two proposed products may act as strong anti-Alzheimer leads compounds

Current Issues in Pharmacy and Medical Sciences published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics