Month: February 2023

Aloe-emodin, a naturally occurring anthraquinone, is a highly potent mast cell stabilizer through activating mitochondrial calcium uniporter was written by Gao, Yuan;Zhang, Xiaoyu;Li, Ximeng;Qi, Ruijuan;Han, Yixin;Kang, Yuan;Cai, Runlan;Peng, Cheng;Qi, Yun. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2021.Product Details of 53902-12-8 This article mentions the following:

Mast cells play a fundamental role in immune system. Upon stimulation, they are activated via IgE dependent or independent pathway and then release granules which contain plenty of preformed constituents. Mast cell stabilizers are commonly used clin. for inhibiting the degranulation of mast cells. In the current study, we firstly identified aloe-emodin, a naturally occurring anthraquinone, was a prominent mast cell stabilizer. It could strikingly dampen IgE/FcεRI- and MAS-related G protein coupled receptor (Mrgpr)-mediated mast cell degranulation in vitro and in vivo. Mechanism study indicated that aloe-emodin rapidly and reversibly decreased cytosolic Ca2+ (Ca2+[c]) concentration through enhancing the mitochondrial Ca2+ (Ca2+[m]) uptake. After genetically silencing or pharmacol. inhibiting mitochondrial calcium uniporter (MCU), the effects of aloe-emodin on the Ca2+[c] level and mast cell degranulation were significantly weakened. In contrast to six clin. drugs with mast cell stabilizing properties (amlexanox, tranilast, ketotifen, cromolyn disodium salt, dexamethasone and pimecrolimus), aloe-emodin showed an impressive and potent inhibitory action on the mast cell degranulation. Collectively, aloe-emodin is a highly potent mast cell stabilizer. By directly activating MCU, it decreases Ca2+[c] level to suppress mast cell degranulation. Our study may provide a promising candidate for the treatment of mast cell activation-related diseases. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Product Details of 53902-12-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Asymmetric Copper-Catalyzed Intermolecular Aminoarylation of Styrenes: Efficient Access to Optical 2,2-Diarylethylamines was written by Wang, Dinghai;Wu, Lianqian;Wang, Fei;Wan, Xiaolong;Chen, Pinhong;Lin, Zhenyang;Liu, Guosheng. And the article was included in Journal of the American Chemical Society in 2017.Related Products of 5339-69-5 This article mentions the following:

We have developed a copper-catalyzed enantioselective intermol. aminoarylation of alkenes using a novel N-fluoro-N-alkylsulfonamide as the amine reagent, which could react with the Cu(I) catalyst to release a related amino radical. After addition to styrene, the generated benzylic radical could couple with a chiral L*Cu^IIAr complex to achieve enantioselective arylation. Various optical 2,2-diarylethylamines were efficiently synthesized from simple styrenes with high enantioselectivity, and these products can serve as valuable synthons toward bioactive mols.’ synthesis. In the experiment, the researchers used many compounds, for example, N-Isopropylbenzenesulfonamide (cas: 5339-69-5Related Products of 5339-69-5).

N-Isopropylbenzenesulfonamide (cas: 5339-69-5) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Related Products of 5339-69-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Development of [¹⁸F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging was written by Hu, Kongzhen;Patnaik, Debasis;Collier, Thomas Lee;Lee, Katarzyna N.;Gao, Han;Swoyer, Matthew R.;Rotstein, Benjamin H.;Krishnan, Hema S.;Liang, Steven H.;Wang, Jin;Yan, Zhiqiang;Hooker, Jacob M.;Vasdev, Neil;Haggarty, Stephen J.;Ngai, Ming-Yu. And the article was included in ACS Medicinal Chemistry Letters in 2017.Computed Properties of C8H8ClNO This article mentions the following:

Dysregulation of glycogen synthase kinase-3β (GSK-3β) is implicated in the pathogenesis of neurodegenerative and psychiatric disorders. Thus, development of GSK-3β radiotracers for positron emission tomog. (PET) imaging is of paramount importance, because such a noninvasive imaging technique would allow better understanding of the link between the activity of GSK-3β and central nervous system disorders in living organisms, and it would enable early detection of the enzyme’s aberrant activity. Herein, we report the synthesis and biol. evaluation of a series of fluorine-substituted maleimide derivatives that are high-affinity GSK-3β inhibitors. Radiosynthesis of a potential GSK-3β tracer [¹⁸F]10a is achieved. Preliminary in vivo PET imaging studies in rodents show moderate brain uptake, although no saturable binding was observed in the brain. Further refinement of the lead scaffold to develop potent [¹⁸F]-labeled GSK-3 radiotracers for PET imaging of the central nervous system is warranted. In the experiment, the researchers used many compounds, for example, 2-(2-Chlorophenyl)acetamide (cas: 10268-06-1Computed Properties of C8H8ClNO).

2-(2-Chlorophenyl)acetamide (cas: 10268-06-1) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Computed Properties of C8H8ClNO

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Palladium-Catalyzed α-Arylation of Vinylogous Esters for the Synthesis of γ,γ-Disubstituted Cyclohexenones was written by Johnson, Thomas;Pultar, Felix;Menke, Friedericke;Lautens, Mark. And the article was included in Organic Letters in 2016.Category: amides-buliding-blocks This article mentions the following:

A palladium-catalyzed α-arylation of cyclic vinylogous esters to form products that are converted in one step to γ-alkyl-γ-aryl-substituted cyclohexenones is reported. This Pd-catalyzed reaction proceeds at room temperature, is generally high-yielding, and uses an amount of a com. available catalyst as low as 0.25 mol %. The scope of aryl bromides is particularly broad, and alkenyl bromides can also be used. This two-step protocol, comprising α-arylation and reductive transposition, can be performed in one pot and is applicable to gram-scale synthesis. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2Category: amides-buliding-blocks).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Visible light-driven [3 + 3] annulation reaction of 2H-azirines with Huisgen zwitterions and synthesis of 1,2,4-triazines was written by Cao, Shixuan;Tang, Tong;Li, Jiatian;He, Zhengjie. And the article was included in Organic Chemistry Frontiers in 2022.Recommanded Product: 116332-61-7 This article mentions the following:

A visible light-driven [3 + 3] annulation reaction of 2H-azirines with in-situ generated Huisgen zwitterions from azodicarboxylates and phosphines was herein described. Under very mild conditions and irradiation of blue LED light, disubstituted 2H-azirines readily undergo a formal [3 + 3] annulation reaction with in-situ generated Huisgen zwitterions, affording polysubstituted dihydro-1,2,4-triazines in 51-97% yields with a broad substrate scope. Mechanistic studies unveil that this annulation reaction proceeded through a cascade sequence of nucleophilic addition, light-driven 1,3-ester migration and aza-Wittig-like cyclization. The light-driven ester migration step was believed to be a photochem. process of an intramol. electron donor-acceptor (EDA) complex. In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7Recommanded Product: 116332-61-7).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Recommanded Product: 116332-61-7

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Dealkenylative Alkynylation Using Catalytic Fe^II and Vitamin C was written by Swain, Manisha;Bunnell, Thomas B.;Kim, Jacob;Kwon, Ohyun. And the article was included in Journal of the American Chemical Society in 2022.Safety of 1,3-Dicyclohexylurea This article mentions the following:

In this paper, synthesis of alkyl-tethered alkynes, e.g. I through ozone-mediated and Fe^II-catalyzed dealkenylative alkynylation of unactivated alkenes in presence of alkynyl sulfones was reported. This one-pot reaction, which employed a combination of a catalytic Fe^II salt and L-ascorbic acid, proceeded under mild conditions with good efficiency, high stereoselectivity, and broad functional group compatibility. In contrast to previous Fe^II-mediated reductive fragmentation of α-methoxyhydroperoxides, Fe^II-catalyzed process was devised through a thorough kinetic anal. of multiple competing radical (redox) pathways. The potential of this dealkenylative alkynylation through multiple post-synthetic transformations and late-stage diversifications of complex mols., including natural products and pharmaceuticals was highlighted. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Safety of 1,3-Dicyclohexylurea).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Safety of 1,3-Dicyclohexylurea

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Study of self-association of benzenesulfonamides in carbon tetrachloride by the NMR method was written by Krasnogorskaya, N. N.;Shcherbakova, E. S.;Gur’yanova, E. N.;Gabdikeeva, A. R.;Poletaeva, M. G.. And the article was included in Zhurnal Prikladnoi Spektroskopii in 1989.Related Products of 5339-69-5 This article mentions the following:

Self-association of title compounds PhSO₂NHR (R = Bu, Me₂CH) in CCl₄ was studied by ¹H NMR. It occurs via intermol. NH···O hydrogen bonds. The degree of self-association increases with concentration and decreases with a rise in temperature Thermodn. parameters for associated mols. were determined In the experiment, the researchers used many compounds, for example, N-Isopropylbenzenesulfonamide (cas: 5339-69-5Related Products of 5339-69-5).

N-Isopropylbenzenesulfonamide (cas: 5339-69-5) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Related Products of 5339-69-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of TAED/H₂O₂ system for low temperature bleaching of crude cellulose extracted from jute fiber was written by Wen, Zuoqiang;Zou, Linbo;Wang, Weiming. And the article was included in IOP Conference Series: Materials Science and Engineering in 2018.Category: amides-buliding-blocks This article mentions the following:

Tetraacetylethylenediamine (TAED) activated hydrogen peroxide system had been applied for bleaching of crude cellulose extracted from jute fiber. Comparing with conventional hydrogen peroxide bleaching system, those results showed that bleaching temperature and time could be effectively reduced, and a preferable whiteness could be produced under faint alk. condition. And the optimum conditions for activated bleaching system could be summarized as molar ratio of H₂O₂/TAED 1:0.7, pH 8, pure hydrogen peroxide 0.09 mol/L, temperature 70°C and time 60min. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Category: amides-buliding-blocks).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Imino exchange reaction in a dearomatization strategy: synthesis of N-acyl diarylamines and phenothiazines from two anilines was written by Zhang, Li;Wang, Huiqing;Yang, Bo;Fan, Renhua. And the article was included in Organic Chemistry Frontiers in 2014.Quality Control of N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide This article mentions the following:

N-Sulfonyl cyclohexadienimines generated from an iodine(III)-induced oxidative dearomatization of N-sulfonyl protected para-substituted anilines are ready to undergo an imino exchange reaction with another aniline, which provides an alternative way to access N-acyl diarylamines and phenothiazines. In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6Quality Control of N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Quality Control of N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Human health and ecological risk assessment of 98 pharmaceuticals and personal care products (PPCPs) detected in Indian surface and wastewaters was written by Sengar, Ashish;Vijayanandan, Arya. And the article was included in Science of the Total Environment in 2022.Formula: C23H28ClN3O5S This article mentions the following:

The release of pharmaceuticals and personal care products (PPCPs) in environmental waters has become an urgent issue due to their pseudo-persistent traits. The present study was undertaken to conduct a screening-level risk assessment of 98 PPCPs, detected in different water matrixes (treated wastewater, surface water, and groundwater) of India, for evaluating ecol. risk (risk to fish, daphnia, and algae), human health risk, and antimicrobial resistance (AMR) selection risk by following risk quotient (RQ) based methodol. In the present study, 47% of the detected PPCPs in Indian waters were found to exert a possible risk (RQ > 1) to either aquatic species and human health, or cause AMR selection risk. 17 out of 25 antibiotics detected in the environmental waters were found to pose a threat of AMR selection. 11 out of 49 pharmaceuticals were found to exert human health risk from ingesting contaminated surface water, whereas only 2 pharmaceuticals out of 25 were found to exert risk from the intake of groundwater. Very high RQs (>1000) for few pharmaceuticals were obtained, signifying a great potential of the detected PPCPs in causing severe health concern, aquatic toxicity, and AMR spread. Within India, special attention needs to be given to the pharmaceutical hubs, as the environmental waters in these regions were found to be severely contaminated with drug residues resulting in extremely high RQs. The present study will be helpful in prioritizing the detected PPCPs in the environmental waters of India, for which immediate attention and enforceable guidelines are required. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Formula: C23H28ClN3O5S).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Formula: C23H28ClN3O5S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics