Month: February 2023

Characterization of the vasodilator effect of eugenol in isolated human umbilical cord arteries was written by Dantas, Debora de Menezes;Silva, Andressa de Alencar;Pereira-de-Morais, Luis;Bastos, Carla Mikevely de Sena;Calixto, Gabriela Lucena;Kerntopf, Marta Regina;Menezes, Irwin Rose Alencar de;Weinreich, Daniel;Barbosa, Roseli. And the article was included in Chemico-Biological Interactions in 2022.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Eugenol (EUG) is a phenylpropanoid widely used in the food and cosmetic industries. It is commonly referred to in the literature by its biol. activities such as antioxidant, anti-inflammatory, antimicrobial, and relaxing in organs of laboratory animals, especially in rodent vessels. However, its vasorelaxant potential in human tissue, has not been investigated. Thus, this study characterizes the vasodilatory effect of EUG in the human umbilical artery (HUA). HUAs were isolated, cleaned, sectioned (3-4 mm) and placed in an organ bath (10 mL Krebs Henseleit, 37°C; and carbogenic mixture). EUG (100-1400μM), obtained total relaxation of electromech. contractions induced by KCl (60 mM), and pharmacomech. contractions (30-1200μM), induced by serotonin (10μM) and by histamine (10μM), showing statistically significant concentrations: 600μM, 400μM and 200μM, and EC50 values: 759.8 ± 6.5μM, 229.9 ± 7.9 and 279.0 ± 3.4μM, resp. EUG (1200 and 1400μM) prevented the contraction promoted by BaCl2 (0.1-30 mM), similar to the effects of nifedipine (10μM), sugesting the involvement of EUG in blocking VOCCs. In the presence of tetraethylammonium (10μM), EUG (30-1200μM) did not produce a total relaxation (88.6%), suggesting that an alternative pathway where potassium channels, may partially mediate EUG effect. In the presence of 4-aminopyridine (1 mM), glibenclamide (10μM), and tetraethylammonium (1 mM), EUG relaxed HUAs 100%, although the pharmacol. potency was statistically altered, demonstrating the participation of K+ channels (Kv, KATP, BKCa). Our data indicates that EUG has a vasorelaxant effect on HUAs, had a greater pharmacol. potency in the serotoninergic pathway, showing effective participation of VOCCs and a partial modulation of K+ channels. These data suggest new possibilities for the use of EUG in human vascular dysfunctions, such as preeclampsia. More studies are necessary to confirm the safety and effectivity in future treatments. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

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.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

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

Organic ligand and solvent free oxidative carbonylation of amine over Pd/TiO₂ with unprecedented activity was written by Liu, Shujuan;Dai, Xingchao;Wang, Hongli;Shi, Feng. And the article was included in Green Chemistry in 2019.Recommanded Product: 2387-23-7 This article mentions the following:

A highly active Pd/TiO₂ catalyst system was prepared and applied in the oxidative carbonylation of amines to ureas with ultra-low Pd content under organic ligand and solvent free conditions. The catalytic turnover frequencies (TOFs, moles of amines converted per mol of Pd per h) were 126 000 and 250 000 h^-1 for the production of diphenylurea and dibenzylurea, resp. An expanded substrate scope including the electron-rich and electron-deficient anilines, primary aliphatic amines, secondary amines was also established. This work offers a straightforward, step economic, and green methodol. for the efficient synthesis of valuable ureas. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Recommanded Product: 2387-23-7).

1,3-Dicyclohexylurea (cas: 2387-23-7) 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. 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.Recommanded Product: 2387-23-7

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

On the Synthesis and Reactivity of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones was written by Sutherell, Charlotte L.;Ley, Steven V.. And the article was included in Synthesis in 2017.Name: 6-Chloro-2-aminobenzamide This article mentions the following:

An improved, scalable synthetic route to the quinazolinone natural product 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one I (R = H, 6-F, 7-OMe, 8-Me, etc.) is reported. The applicability of this method to analog synthesis and the synthesis of related natural products are explored. Finally, reactivity of the scaffold to a variety of electrophilic reagents, generating products stereoselectively, e.g., II, is reported. In the experiment, the researchers used many compounds, for example, 6-Chloro-2-aminobenzamide (cas: 54166-95-9Name: 6-Chloro-2-aminobenzamide).

6-Chloro-2-aminobenzamide (cas: 54166-95-9) 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.Name: 6-Chloro-2-aminobenzamide

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

Synthesis of naphtho[2,3-b]pyrandiones: (-)-cryptosporin was written by Brade, Walter;Vasella, Andrea. And the article was included in Helvetica Chimica Acta in 1989.Category: amides-buliding-blocks This article mentions the following:

A new method for the synthesis of naphtho[2,3-b]pyrandiones from sulfonyl lactones and 1-nitroglycals is presented. Thus, 3-phenylsulfonylphthalide (I, R = H) reacted with the 1-nitroglycal II in the presence of LiN(CHMe₂)₂ at room temperature to give the naphthopyrandione III in high yields. Reaction at a lower temperature led to the intermediate Michael-addition products. I (R = OCH₂OCH₂CH₂OMe) and the 1-nitroglycal IV were prepared for the synthesis of the title compound (V) by base-promoted condensation and deblocking. In the experiment, the researchers used many compounds, for example, N,N-Diethylsalicylamide (cas: 19311-91-2Category: amides-buliding-blocks).

N,N-Diethylsalicylamide (cas: 19311-91-2) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Category: amides-buliding-blocks

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

Cu(II)-metformin immobilized on graphene oxide: an efficient and recyclable catalyst for the Beckmann rearrangement was written by Solaiman Hamed, Ahmed;Mohammad Ali, Ehab. And the article was included in Research on Chemical Intermediates in 2020.Recommanded Product: 2670-38-4 This article mentions the following:

In this study, for the first time, the copper(II) nanoparticles (NPs) have been immobilized on metformin-functionalized graphene oxide and then its catalytic applications have been investigated in synthesis of amides from aldoximes (Beckmann rearrangement). All analyses confirm the successful and stable immobilization of copper NPs on functionalized graphene oxide. This synthesized heterogeneous nanocatalyst showed excellent catalytic activity with high product yields and short reaction times. Also, the suggested catalyst could be recycled ten times without a drastic decrease in its catalytic activity. In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Recommanded Product: 2670-38-4).

3,4-Dichlorobenzamide (cas: 2670-38-4) 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.Recommanded Product: 2670-38-4

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

In vivo antihyperglycaemic and antihyperlipidemic activities and chemical constituents of Solanum anomalum was written by Okokon, Jude E.;Etuk, Idongesit C.;Thomas, Paul S.;Drijfhout, Falko P.;Claridge, Tim D. W.;Li, Wen-Wu. And the article was included in Biomedicine & Pharmacotherapy in 2022.Related Products of 10238-21-8 This article mentions the following:

Solanum anomalum is a plant used ethnomedically for the treatment of diabetes. The study was aimed to validate ethnomedical claims in rat model and identify the likely antidiabetic compounds Leaf extract (70-210 mg/kg/day) and fractions (140 mg/kg/day) of S. anomalum were evaluated in hyperglycemic rats induced using alloxan for effects on blood glucose, lipids and pancreas histol. Phytochem. characterization of isolated compounds and their identification were performed using mass spectrometry and NMR spectroscopy. Bioinformatics tool was used to predict the possible protein targets of the identified bioactive compounds The leaf extract/fractions on administration to diabetic rats caused significant lowering of fasting blood glucose of the diabetic rats during single dose study and on repeated administration of the extract The hydroethanolic leaf extracts also enhanced glucose utilization capacity of the diabetic rats and caused significant lowering of glycosylated Hb levels and elevation of insulin levels in the serum. Furthermore, triglycerides, LDL-cholesterol, and VLDL-cholesterol levels were lowered significantly, while HDL-cholesterol levels were also elevated in the treated diabetic rats. There was absence or few pathol. signs in the treated hyperglycemic rat pancreas compared to that present in the pancreas of control group. Diosgenin, 25(R)-diosgenin-3-O-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranoside, uracil, thymine, 1-octacosanol, and octacosane were isolated and identified. Protein phosphatases along with secreted proteins are predicted to be the major targets of diosgenin and the diosgenin glycoside. These results suggest that the leaf extract/fractions of S. anomalum possess antidiabetic and antihyperlipidemic properties, offer protection to the pancreas and stimulate insulin secretion, which can be attributable to the activities of its phytochem. constituents. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Related Products of 10238-21-8).

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. 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 10238-21-8

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

Application of a novel prioritisation strategy using non-target screening for evaluation of temporal trends (1969-2017) of contaminants of emerging concern (CECs) in archived lynx muscle tissue samples was written by Durig, Wiebke;Alygizakis, Nikiforos A.;Wiberg, Karin;Ahrens, Lutz. And the article was included in Science of the Total Environment in 2022.Recommanded Product: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Most environmental monitoring studies of contaminants of emerging concern (CECs) focus on aquatic species and target specific classes of CECs. Even with wide-scope target screening methods, relevant CECs may be missed. In this study, non-target screening (NTS) was used for tentative identification of potential CECs in muscle tissue of the terrestrial top predator Eurasian lynx (Lynx lynx). Temporal trend anal. was applied as a prioritisation tool for archived samples, using univariate statistical tests (Mann-Kendall and Spearman rank). Pooled lynx muscle tissue collected from 1969 to 2017 was analyzed with an eight-point time series using a previously validated screening workflow. Following peak detection, peak alignment, and blank subtraction, 12,941 features were considered for statistical anal. Prioritisation by time-trend anal. detected 104 and 61 features with statistically significant increasing and decreasing trends, resp. Following probable mol. formula assignment and elucidation with MetFrag, two compounds with increasing trends, and one with a decreasing trend, were tentatively identified. These results show that, despite low expected concentration levels and high matrix effects in terrestrial species, it is possible to prioritise CECs in archived lynx samples using NTS and univariate statistical approaches. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Recommanded Product: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) 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. 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.Recommanded Product: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

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

Cu₂O-Catalyzed Conversion of Benzyl Alcohols Into Aromatic Nitriles via the Complete Cleavage of the C≡N Triple Bond in the Cyanide Anion was written by Liu, Wenbo;Tang, Peichen;Zheng, Yi;Ren, Yun-Lai;Tian, Xinzhe;An, Wankai;Zheng, Xianfu;Guo, Yinggang;Shen, Zhenpeng. And the article was included in Chemistry – An Asian Journal in 2021.Formula: C7H5Cl2NO This article mentions the following:

Nitrogen transfer from cyanide anion to an aldehyde is emerging as a promising method for the synthesis of aromatic nitriles. However, this method still suffers from a disadvantage that a use of stoichiometric Cu(II) or Cu(I) salts is required to enable the reaction. As authors report herein, overcame this drawback and developed a catalytic method for nitrogen transfer from cyanide anion to an alc. via the complete cleavage of the C≡N triple bond using phen/Cu₂O as the catalyst. The present condition allowed a series of benzyl alcs. to be smoothly converted into aromatic nitriles in moderate to high yields. In addition, the present method could be extended to the conversion of cinnamic alc. to 3-phenylacrylonitrile. In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Formula: C7H5Cl2NO).

3,4-Dichlorobenzamide (cas: 2670-38-4) 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 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.Formula: C7H5Cl2NO

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

Age-Related Changes in the Functional Activity of ATP-Sensitive Potassium Channels in Rat Pial Arteries was written by Gorshkova, O. P.. And the article was included in Journal of Evolutionary Biochemistry and Physiology in 2022.Quality Control of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Age-related changes in the contribution of ATP-sensitive potassium channels (K_ATP) to basal tone and acetylcholine (ACh)-mediated dilation of pial arterial vessels were studied in Wistar rats aged 4 and 18 mo using intravital microphotog. A change in the contribution of K_ATP channels to the maintenance of basal tone was assessed by the change in the number of vessels constricted in response to a K_ATP channel blocker glibenclamide (10 μM). A change in the contribution of K_ATP channels to vasodilation was assessed by comparing the number and degree of arterial dilation in response to ACh (10^-7 M, 5 min) before and after glibenclamide application. It was found that aging is accompanied by a decrease in the contribution of K_ATP channels to basal tone of pial arteries. Moreover, the functional activity of K_ATP channels and their contribution to vasodilation decreases with age, and in 18-mo-old rats they are practically not involved in the dilatory response to ACh. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Quality Control of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Quality Control of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

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

Amine-Responsive Disassembly of Au^I-Cu^I Double Salts for Oxidative Carbonylation was written by Cao, Yanwei;Yang, Jian-Gong;Deng, Yi;Wang, Shengchun;Liu, Qi;Shen, Chaoren;Lu, Wei;Che, Chi-Ming;Chen, Yong;He, Lin. And the article was included in Angewandte Chemie, International Edition in 2020.Application In Synthesis of 1,3-Dicyclohexylurea This article mentions the following:

A sensitive amine-responsive disassembly of self-assembled Au^I-Cu^I double salts was observed and its use for the synergistic catalysis was enlightened. Study of the disassembly of [Au(NHC)₂][CuI₂] revealed the contribution of Cu-assisted ligand exchange of N-heterocyclic carbene (NHC) by amine in [Au(NHC)₂]⁺ and the capacity of [CuI₂]^– on the oxidative step. By integrating the implicative information coded in the responsive behavior and inherent catalytic functions of d¹⁰ metal complexes, a catalyst for the oxidative carbonylation of amines was developed. The advantages of this method were clearly reflected on mild reaction conditions and the significantly expanded scope (51 examples); both primary and steric secondary amines can be employed as substrates. The cooperative reactivity from Au and Cu centers, as an indispensable prerequisite for the excellent catalytic performance, was validated in the synthesis of (un)sym. ureas and carbamates. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Application In Synthesis of 1,3-Dicyclohexylurea).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Application In Synthesis of 1,3-Dicyclohexylurea

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