Tag: 400-500

Methotrexate analogs. 9. Synthesis and biological properties of some 8-alkyl-7,8-dihydro analogs was written by Chaykovsky, Michael;Hirst, Margaret;Lazarus, Herbert;Martinelli, Jack E.;Kisliuk, Roy L.;Gaumont, Yvette. And the article was included in Journal of Medicinal Chemistry in 1977.COA of Formula: C20H20N8Na2O5 This article mentions the following:

Eight title derivatives were prepared by direct alkylation of 7,8-dihydromethotrexate (I) [14009-31-5]. I and 8-methyl-7,8-dihydromethotrexate (II) [54820-64-3] were comparable to methotrexate (MTX) in their inhibition of Lactobacillus casei growth. I and all its derivatives were less inhibitory toward dihydrofolate reductase [9002-03-3] than MTX, but all were more inhibitory towared thymidylate synthetase [9031-61-2] from L. casei. I was about as active as MTX in vitro against CCRF-CEM human lymphoblastic cells, but was inactive against L1210 leukemia in mice. The 8-alkyl derivatives of I were much less toxic than I, and several derivatives had some in vivo activity against L1210 leukemia. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5COA of Formula: C20H20N8Na2O5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) 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. 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.COA of Formula: C20H20N8Na2O5

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

Identification of transporters associated with etoposide sensitivity of stomach cancer cell lines and methotrexate sensitivity of breast cancer cell lines by quantitative targeted absolute proteomics was written by Obuchi, Wataru;Ohtsuki, Sumio;Uchida, Yasuo;Ohmine, Ken;Yamori, Takao;Terasaki, Tetsuya. And the article was included in Molecular Pharmacology in 2013.Computed Properties of C20H20N8Na2O5 This article mentions the following:

Membrane transporter proteins may influence the sensitivity of cancer cells to anticancer drugs that can be recognized as substrates. The purpose of this study was to identify proteins that play a key role in the drug sensitivity of stomach and breast cancer cell lines by measuring the absolute protein expression levels of multiple transporters and other membrane proteins and examining their correlation to drug sensitivity. Absolute protein expression levels of 90 membrane proteins were examined by quant. targeted absolute proteomics using liquid chromatog.-linked tandem mass spectrometry. Among them, 11 and 14 membrane proteins, including transporters, were present in quantifiable amounts in membrane fraction of stomach cancer and breast cancer cell lines, resp. In stomach cancer cell lines, the protein expression level of multidrug resistance-associated protein 1 (MRP1) was inversely correlated with etoposide sensitivity. MK571, an MRP inhibitor, increased both the cell-to-medium ratio of etoposide and the etoposide sensitivity of MRP1-expressing stomach cancer cell lines. In breast cancer cell lines, the protein expression level of reduced folate carrier 1 (RFC1) was directly correlated with methotrexate (MTX) sensitivity. Initial uptake rate and steady-state cell-to-medium ratio of [³H]MTX were correlated with both RFC1 expression level and MTX sensitivity. These results suggest that MRP1 modulates the etoposide sensitivity of stomach cancer cell lines and RFC1 modulates the MTX sensitivity of breast cancer cell lines. Our results indicate that absolute quantification of multiple membrane proteins could be a useful strategy for identification of candidate proteins involved in drug sensitivity. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Computed Properties of C20H20N8Na2O5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) 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. 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.Computed Properties of C20H20N8Na2O5

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

Dose-dependent Spasmolytic, Bronchodilator, and Hypotensive Activities of Panicum miliaceum L. was written by Saqib, Fatima;Al-Huqail, Arwa Abdulkreem;Asma, Memona;Chicea, Liana;Hogea, Mircea;Irimie, Marius;Gavris, Claudia. And the article was included in Dose-Response in 2022.Recommanded Product: 10238-21-8 This article mentions the following:

Panicum miliaceum L. is a medicinally effective plant used in indigenous system of medicine for a variety of ailments. However, there is no comprehensive study explaining its effectiveness in gastrointestinal tract, respiratory, and cardiovascular system ailments. This study was designed to validate the pharmacol. basis for the folkloric use of Panicum miliaceum L. in diarrhea, asthma, and hypertension. Panicum miliaceum extract was analyzed to detect the presence of bioactive compounds by HPLC. The isolated rabbit jejunum, trachea, and aorta were used for in vitro experiments using tissue bath assembly coupled with Power Lab data acquisition system to explore their relative effects. In-vivo experiments were performed for anti-diarrheal activity. HPLC anal. revealed the presence of gallic acid, butylated hydroxytoluene, catechin, and quercetin. Concentration dependent activities were observed by relaxing K⁺ (low) induced contractions having spasmolytic effect with EC50 = .358 ± .052, bronchodilator (EC50 = 2.483 ± .05793), and vasorelaxant (EC50 = .383 ± .063), probably due to the ATP dependent potassium channel activation. It was confirmed through pre-exposure of glibenclamide (specific ATP-dependent K⁺ channel blocker) having similarities with cromakalim. Pm. Cr revealed its antidiarrheal via in vivo experiments on rats. This study indicates that Panicum miliaceum has antidiarrheal, spasmolytic, bronchodilator, and vasorelaxant activities probably due to the ATP dependent K⁺ channel activation. 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: 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. 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: 10238-21-8

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

Characterization of the contamination fingerprint of wastewater treatment plant effluents in the Henares River Basin (central Spain) based on target and suspect screening analysis was written by Lopez-Herguedas, N.;Gonzalez-Gaya, B.;Castelblanco-Boyaca, N.;Rico, A.;Etxebarria, N.;Olivares, M.;Prieto, A.;Zuloaga, O.. And the article was included in Science of the Total Environment in 2022.Reference of 10238-21-8 This article mentions the following:

The interest in contaminants of emerging concern (CECs) has increased lately due to their continued emission and potential ecotoxicol. hazards. Wastewater treatment plants (WWTPs) are generally not capable of eliminating them and are considered the main pathway for CECs to the aquatic environment. The number of CECs in WWTPs effluents is often so large that complementary approaches to the conventional target anal. need to be implemented. Within this context, multitarget quant. anal. (162 compounds) and a suspect screening (>40,000 suspects) approaches were applied to characterize the CEC fingerprint in effluents of five WWTPs in the Henares River basin (central Spain) during two sampling campaigns (summer and autumn). The results indicated that 76% of the compounds quantified corresponded to pharmaceuticals, 21% to pesticides and 3% to industrial chems. Apart from the 82 compounds quantified, suspect screening increased the list to 297 annotated compounds Significant differences in the CEC fingerprint were observed between summer and autumn campaigns and between the WWTPs, being those serving the city of Alcala de Henares the ones with the largest number of compounds and concentrations Finally, a risk prioritization approach was applied based on risk quotients (RQs) for algae, invertebrates, and fish. Azithromycin, diuron, chlortoluron, clarithromycin, sertraline and sulfamethoxazole were identified as having the largest risks to algae. As for invertebrates, the compounds having the largest RQs were carbendazim, fenoxycarb and eprosartan, and for fish acetaminophen, DEET, carbendazim, caffeine, fluconazole, and azithromycin. The two WWTPs showing higher calculated Risk Indexes had tertiary treatments, which points towards the need of increasing the removal efficiency in urban WWTPs. Furthermore, considering the complex mixtures emitted into the environment and the low dilution capacity of Mediterranean rivers, we recommend the development of detailed monitoring plans and stricter regulations to control the chem. burden created to freshwater ecosystems. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Reference of 10238-21-8).

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

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

The screening of emerging micropollutants in wastewater in Sol Plaatje Municipality, Northern Cape, South Africa was written by Oluwalana, Abimbola E.;Musvuugwa, Tendai;Sikwila, Stephen T.;Sefadi, Jeremia S.;Whata, Albert;Nindi, Mathew M.;Chaukura, Nhamo. And the article was included in Environmental Pollution (Oxford, United Kingdom) in 2022.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Although pollutants pose environmental and human health risks, the majority are not routinely monitored and regulated. Organic pollutants emanate from a variety of sources, and can be classified depending on their chem. and environmental fate. Classification of pollutants is important because it informs fate processes and apposite removal technologies. The occurrence of emerging contaminants (ECs) in water bodies is a source of environmental and human health concern globally. Despite being widely reported, data on the occurrence of ECs in South Africa are scarce. Specifically, ECS in wastewater in the Northern Cape in South Africa are understudied. In this study, various ECs were screened in water samples collected from three wastewater treatment plants (WWTPs) in the province. The ECs were detected using liquid chromatog. coupled to high resolution Orbitrap mass spectrometry following Oasis HLB solid-phase extraction The main findings were: (1) there is a wide variety of ECs in the WWTPs, (2) physico-chem. properties such as pH, total dissolved solids, conductivity, and dissolved organic content showed reduced values in the outlet compared to the inlet which confirms the presence of less contaminants in the treated wastewater, (3) specific UV absorbance of less than 2 was observed in the WWTPs samples, suggesting the presence of natural organic matter (NOM) that is predominantly non-humic in nature, (4) most of the ECs were recalcitrant to the treatment processes, (5) pesticides, recreational drugs, and analgesics constitute a significant proportion of pollutants in wastewater, and (6) NOM removal ranged between 35 and 90%. Consequently, a comprehensive database of ECs in wastewater in Sol Plaatje Municipality was created. Since the detected ECs pose ecotoxicol. risks, there is a need to monitor and quantify ECs in WWTPs. These data are useful in selecting suitable monitoring and control strategies at WWTPs. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Safety 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. 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 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.Safety of 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

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

Hypoglycemic, hypolipidemic and hepatoprotective effects of Alpinia officinarum on nicotinamide/streptozotocin induced type II diabetic rats. was written by Heidari, Hamid;Khalaj, Azam;Khani, Sima;Abdollahi, Maasoume;Farahani, Hamid;Khani, Samira. And the article was included in Hormone molecular biology and clinical investigation in 2022.Reference of 10238-21-8 This article mentions the following:

OBJECTIVES: Alpinia officinarum Hance, commonly known as lesser galangal, is a member of the ginger family (Zingiberaceae) traditionally used for many decades to treat inflammation, pain, stomach ache and cold. In the present study, the antidiabetic and hypolipidemic potentials of the hydroalcoholic extract of A. officinarum (AO) were investigated in the nicotinamide/streptozotocin induced type II diabetic rats. METHODS: Male Wistar rats were divided into following six groups: Group I was normal control rats. Group II: normal diabetic control, Group III: Diabetic rats treated with glibenclamide (0.25 mg/kg), IV, V and VI: Diabetic rats treated with 100, 200 and 500 mg/kg AO hydroalcoholic extract by daily gavage for 28 days, respectively. At the end of treatment, biochemical analysis, histological study, phytochemical analysis and acute toxicity tests were carried out. RESULTS: The results show significant reduction in blood glucose, serum lipid profiles, and liver enzyme levels in diabetic rats compared with diabetic control in AO treated group. CONCLUSIONS: In conclusion, the present study demonstrated that AO extract had significant (p<0.05) antidiabetic and anti-hyperlipidemia effects in addition to hepatoprotective effect in type II diabetic rats. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Reference of 10238-21-8).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) 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. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Reference of 10238-21-8

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

A convenient preparation of tetrahydropteridines and tetrahydrofolate analogs. Synthesis of tetrahydro-3′,5′-dichloromethotrexate was written by Martinelli, Jack E.;Chaykovsky, Michael. And the article was included in Preparative Biochemistry in 1980.Application In Synthesis of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate This article mentions the following:

Folic acid (I; R = OH, R¹ = R² = H), methotrexate (I; R = NH₂, R¹ = Me, R² = H), and 3′,5′-dichloromethotrexate (I; R = NH₂, R¹ = Me, R² = Cl) were reduced by Me₂NH/borane at 20-60° to give the corresponding tetrahydropteridines II. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Application In Synthesis of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) 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. 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.Application In Synthesis of Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate

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

Quantification of drugs encapsulated in liposomes by ¹H NMR was written by Guimaraes, Diana;Noro, Jennifer;Loureiro, Ana;Cavaco-Paulo, Artur;Nogueira, Eugenia. And the article was included in Colloids and Surfaces, B: Biointerfaces in 2019.HPLC of Formula: 7413-34-5 This article mentions the following:

Liposomes are one of the most important and extensively studied drug delivery system due to their ability to encapsulate different kinds of drugs. Exploiting the advantages of ¹H NMR (NMR) spectrometry, we established a rapid and easy method for quantification of drugs encapsulated in liposomes. An internal standard, pyridine, was used for quant. determination of drug concentration Two different drugs were involved in this work, one hydrophilic, methotrexate disodium salt, and another hydrophobic, tamoxifen. The specificity and selectivity of the suggested method were evaluated by the absence of overlapping of at least one signal of each drug with pyridine in the NMR spectrum. The accuracy and precision of the method were assessed by adding a known amount of each drug to unloaded liposomes. Results obtained by quant. NMR (qNMR) were validated and confirmed by comparing with two other traditional techniques, UV-Visible (UV-vis) spectrophotometry and High-Performance Liquid Chromatog. (HPLC). It was found that the results were consistent with the ones obtained from our proposed qNMR method. Considering all the experiments conducted in this study, we deliberate that qNMR can be a suitable tool for the determination of drugs encapsulated in liposomes. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5HPLC of Formula: 7413-34-5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) 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. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.HPLC of Formula: 7413-34-5

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

Aristolone in Nardostachys jatamansi DC. induces mesenteric vasodilation and ameliorates hypertension via activation of the K_ATP channel and PDK1-Akt-eNOS pathway was written by Fang, Jingmei;Li, Ran;Zhang, Yue;Oduro, Patrick Kwabena;Li, Sa;Leng, Ling;Wang, Zhimei;Rao, Yao;Niu, Lu;Wu, Hong-Hua;Wang, Qilong. And the article was included in Phytomedicine in 2022.Application of 10238-21-8 This article mentions the following:

Nardostachys jatamansi DC. is a common medicinal herb used to treat cardiovascular diseases, particularly hypertension. Previously, our lab characterized the chem. compounds of N. jatamansi. However, the bioactive compounds of N. jatamansi and their mechanisms of action on blood pressure and blood vessels are unknown. The vasorelaxant effects of the methanolic extract (MeOH extract) of the roots and rhizomes of N. jatamansi, its main compounds, and their underlying mode of action, were investigated.The main compounds of N. jatamansi were isolated and identified using UHPLC-TOF MS. The antihypertensive effect of N. jatamansi extracts and (-)-aristolone were determined using spontaneously hypertensive rats. The extracts, fractions, and compounds were also evaluated for their vasorelaxant effects on U46619 contractile responses in isolated thoracic aortic and mesenteric arterial rings. The endothelial-dependent relaxation, as well as the regulatory pathways and targets of (-)-aristolone, were studied in-vitro and ex-vivo. Mol. docking and biophys. characterization (Surface plasmon resonance) studies were utilized to investigate the mol. interaction between (-)-aristolone and the target protein.MeOH extract (200 mg/kg) reduces the systolic and diastolic blood pressure in spontaneously hypertensive rats. MeOH extract and its Et acetate fraction (EtOAc Fr.), but not the H2O fraction, had a significant relaxing effect on the thoracic aorta. (-)-aristolone and kanshone H from EtOAc Fr. induced vasorelaxation of the thoracic aorta and mesenteric artery. In human umbilical vein endothelial cells, (-)-aristolone treatment upregulated phosphorylation of Akt (T308) and eNOS. Mol. docking and surface plasmon resonance experiments revealed an interaction between (-)-aristolone and phosphoinositide-dependent protein kinase 1 (PDK1), an upstream protein kinase that phosphorylates Akt at T308. Treatment with PDK1 inhibitor PHT-427 and eNOS inhibitor L-NAME consistently inhibited (-)-aristolone-induced vasorelaxation. In addition, KATP channel inhibitor glibenclamide dramatically inhibited the vasorelaxant effects of (-)-aristolone and kanshone H in the endothelium-denuded thoracic aorta. Finally, (-)-aristolone lowers hypertensive rats systolic and diastolic blood pressure.The extracts of N. jatamansi promote vasorelaxation and alleviate hypertension. The essential chems. responsible for producing vasorelaxation effects are (-)-aristolone and kanshone H, which activate the PDK1-Akt-eNOS-NO relaxing pathway and stimulate the opening of the KATP channel. These findings point to N. jatamansi and aristolone as possible antihypertensive agents. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Application of 10238-21-8).

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

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

Bridelia ferruginea Benth. (Euphorbiaceae) mitigates oxidative imbalance and lipotoxicity, with concomitant modulation of insulin signaling pathways via GLUT4 upregulation in hepatic tissues of diabetic rats was written by Oyebode, Olajumoke A.;Erukainure, Ochuko L.;Chuturgoon, Anil A.;Ghazi, Terisha;Naidoo, Pragalathan;Chukwuma, Chika I.;Islam, Shahidul Md.. And the article was included in Journal of Ethnopharmacology in 2022.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Bridelia ferruginea Benth. (Euphorbiaceae) is among the medicinal plants commonly used for the management of type 2 diabetes (T2D) and its complications. The hepato-therapeutic effect of the butanol fraction of Bridelia ferruginea leaves was investigated in diabetic rats The butanol fraction of B. ferruginea was given to type 2 diabetic rats at both low and high doses (150 and 300 mg/kg bodyweight, respectivley), while metformin and glibenclamide served as the standard anti-diabetic drugs. A normal toxicol. group was administered a high dose of the fraction. At the end of the expremental period, the rats were sacrificed, and their livers and psoas muscle collected. The liver was assayed for oxidative stress markers, liver glycogen content, lipid metabolite profile (using GC-MS) and their metabolic pathways were analyzed using the MetaboAnalyst 5.0 online server. The expression of GLUT4 was also assayed in the liver and muscle as well as the identification of signaling pathways associated with GLUT4 expression using the Enrichr online server. In silico mol. docking was used to investigate the mol. interactions of some postulated compound found in B. ferruginea with GLUT4. The ability of the fraction to stimulate muscle glucose uptake was determined in isolated rat psoas muscle ex vivo. Treatment with the high dose of fraction caused an inhibition of lipid peroxidation as well as the elevation of catalase, SOD, glutathione reductase and glutathione peroxidase activities in the rat liver. There was an increased expression of GLUT4 in livers and muscles of diabetic rats following treatment with B. ferruginea. Treatment with the fraction also caused inactivation of diabetes-activated pathways and changes in the distribution of the hepatic lipid metabolites. Mol. docking anal. revealed strong mol. interactions of pyrogallol and sitosterol with GLUT4. These data illustrate the hepato-protective effect of B. ferruginea in diabetic rats which compare favorably with the tested anti-diabetic drugs (metformin and glibenclamide). 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. 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′Râ€? or, equivalently, an acyl (alkanoyl) group RC(=O)âˆ?joined to an amine group. The presence of the amide group –C(=O)Nâ€?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 cmâˆ?. 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