Month: November 2022

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

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

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

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

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

Gless, Bengt H. published the artcileIdentification of autoinducing thiodepsipeptides from staphylococci enabled by native chemical ligation, Name: H-Lys(Boc)-OH, the publication is Nature Chemistry (2019), 11(5), 463-469, database is CAplus and MEDLINE.

Staphylococci secrete autoinducing peptides (AIPs) as signaling mols. to regulate population-wide behavior. AIPs from non-Staphylococcusaureus staphylococci have received attention as potential antivirulence agents to inhibit quorum sensing and virulence gene expression in the human pathogen Staphylococcus aureus. However, only a limited number of AIP structures from non-S. aureus staphylococci have been identified to date, as the minute amounts secreted in complex media render it difficult. Here, we report a method for the identification of AIPs by exploiting their thiolactone functionality for chemoselective trapping and enrichment of the compounds from the bacterial supernatant. Standard liquid chromatog. mass spectrometry anal., guided by genome sequencing data, then readily provides the AIP identities. Using this approach, we confirm the identity of five known AIPs and identify the AIPs of eleven non-S. aureus species, and we expect that the method should be extendable to AIP-expressing Gram-pos. bacteria beyond the Staphylococcus genus.

Nature Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

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

Jala, Venkatakrishna R. published the artcileThe yin and yang of leukotriene B₄ mediated inflammation in cancer, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Seminars in Immunology (2017), 58-64, database is CAplus and MEDLINE.

The high affinity leukotriene B₄ receptor, BLT1 mediates chemotaxis of diverse leukocyte subsets to the sites of infection or inflammation. Whereas the pathol. functions of LTB₄/BLT1 axis in allergy, autoimmunity and cardiovascular disorders are well established; its role in cancer is only beginning to emerge. In this review, we summarize recent findings on LTB₄/BLT1 axis enabling distinct outcomes toward tumor progression. In a mouse lung tumor model promoted by silicosis-induced inflammation, genetic deletion of BLT1 attenuated neutrophilic inflammation and tumor promotion. In contrast, in a spontaneous model of intestinal tumorigenesis, absence of BLT1 led to defective mucosal host response, altered microbiota and bacteria dependent colon tumor progression. Furthermore, BLT1 mediated CD8⁺ T cell recruitment was shown to be essential for initiating anti-tumor immunity in number of xenograft models and is critical for effective PD1 based immunotherapy. BLT2 mediated chemotherapy resistance, tumor promotion and metastasis are also discussed. This new information points to a paradigm shift in our understanding of the LTB₄ pathways in cancer.

Seminars in Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Demchenko, Anatoly published the artcileSynthesis and biological activity of new [1,3]Thiazolo[4,5-d]pyridazin-4(5H)-ones, Product Details of C5H10N2OS, the publication is Scientia Pharmaceutica (2016), 84(2), 255-268, database is CAplus and MEDLINE.

A series of novel 2-(N-pyrrolidino, N-piperidino or N-morpholino)-7-phenyl- (α-furoyl or α-thienyl)-[1,3]thiazolo[4,5-d]pyridazinones 10a-c, 14-16a,b was synthesized in 78-87% yields via the reaction of Me 5-benzoyl(α-furoyl or α-thienyl)-2-aminosubstituted-thiazol-4-carboxylates 9a-c, 13a-e with hydrazine. These new compounds have been tested for their in vivo analgesic and anti-inflammatory activities. All compounds have been characterized by 1H- NMR, 13C-NMR spectroscopy, and liquid chromatog.-mass spectrometry.

Scientia Pharmaceutica published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Product Details of C5H10N2OS.

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

Wentrup, Gerhard Juergen published the artcile1,2-Dithiacyclopentenes, XXXII. Reactions of 3H-1,2-dithiole-3-thiones with N-chlorobenzamides, Name: 2,4-Dichlorobenzamide, the publication is Justus Liebigs Annalen der Chemie (1978), 387-97, database is CAplus.

5-Phenyl-3H-1,2-dithiole-3-thione (I) reacted with RCONCl₂ [R = 2-O₂NC₆H₄, 2,4-(O₂N)ClC₆H₃, 2,4- and 2,6-Cl₂C₆H₃] to give II (R as above, R¹ = H, Cl) whereas reaction of I with RCONHCl (R as above) gave III, which, on extrusion of S gave II (R¹ = H).

Justus Liebigs Annalen der Chemie published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H8BFO2, Name: 2,4-Dichlorobenzamide.

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

Tambe, Suparna published the artcileStructure-performance relationships of phenyl cinnamic acid derivatives as MALDI-MS matrices for sulfatide detection, Related Products of amides-buliding-blocks, the publication is Analytical and Bioanalytical Chemistry (2017), 409(6), 1569-1580, database is CAplus and MEDLINE.

A key aspect for the further development of matrix-assisted laser desorption ionization (MALDI)-mass spectrometry (MS) is a better understanding of the working principles of MALDI matrixes. To address this issue, a chem. compound library of 59 structurally related cinnamic acid derivatives was synthesized. Potential MALDI matrixes were evaluated with sulfatides, a class of anionic lipids which are abundant in complex brain lipid mixtures For each matrix relative mean S/N ratios of sulfatides were determined against 9-aminoacridine as a reference matrix using neg. ion mass spectrometry with 355 and 337 nm laser systems. The comparison of matrix features with their corresponding relative mean S/N ratios for sulfatide detection identified correlations between matrix substitution patterns, their chem. functionality, and their MALDI-MS performance. Crystal structures of six selected matrixes provided structural insight in hydrogen bond interactions in the solid state. Principal component anal. allowed the addnl. identification of correlation trends between structural and phys. matrix properties like number of exchangeable protons at the head group, MW, logP, UV-Vis, and sulfatide detection sensitivity.

Analytical and Bioanalytical Chemistry 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 C7H5I2NO3, Related Products of amides-buliding-blocks.

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