Category: amides-buliding-blocks

Acute toxicity of methotrexate and cyclophosphamide in underfed mice was written by Graczyk, Julita. And the article was included in Bromatologia i Chemia Toksykologiczna in 1980.Synthetic Route of C20H20N8Na2O5 This article mentions the following:

The i.p. LD₅₀ values of Na methotrexate (I Na salt) [7413-34-5] and cyclophosphamide (II) [50-18-0] in mice fed normal diets were 122 and 460 mg/kg, resp. In animals maintained on 10 and 4% protein diets, the toxicity of I was increased by 3.5- and 20-fold, resp., and that of II was increased by 4- and 8-fold, resp. At LD₁₀ doses, I and II decreased serum total proteins levels in mice on normal diets from 72.3 to 49.1 and 46.8 g/dm³, resp. The latter result may possibly explain the enhancement of I and II toxicity by protein-deficient diets. 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: 7413-34-5Synthetic Route of C20H20N8Na2O5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. 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.Synthetic Route of C20H20N8Na2O5

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

Antidiabetic activity of Swarna makshika bhasma, Shuddha shilajatu and their combination in Streptozotocin-induced diabetic Wistar rats was written by Sanjeev, Singh;Khemchand, Sharma. And the article was included in International Journal of Research in Ayurveda & Pharmacy in 2022.Product Details of 10238-21-8 This article mentions the following:

Swarna makshika bhasma and Shilajatu are mentioned by Acharya Sushruta in Madhumeha Chikitsa. These two Rasayanas play a role in glucose and insulin metabolism The present study was undertaken to assess the anti-diabetic activity in Wistar strain albino rats, thirty-six in number divided into six groups. Streptozotocin was given to induce diabetes. Glibenclamide was used as a standard control drug. Doses of all drugs in each group were according to an accepted standard Mild diabetic rats (blood sugar > 200 mg/dL) were given medication after their body weight and blood glucose levels were determined The treatment was maintained on days 7, 14, 21, and 28, and biochem. parameters were calculated From the fourth day of Streptozotocin induction of diabetes, Makshika bhasma, Shuddha shilajatu and their combination, Glibenclamide, were given once daily. After administration, the effects of Swarna makshika bhasma, Shuddha shilajatu, and Combination of Makshika bhasma and Shuddha shilajatu on bodyweight were statistically non-significant. However, there was a distinction between the before and after-effects. The most remarkable changes in blood glucose levels were reported for Makshika bhasma, Shuddha shilajatu, and Makshika bhasma with Shuddha shilajatu. To conclude, the Combination of Shilajatu and Makshika bhasma is the most efficient and remarkably therapy alternative in Madhumeha. Their multifaceted impact makes them a viable method in the long-term control of diabetes. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Product Details of 10238-21-8).

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. 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 10238-21-8

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

Machine Learning Enabled Structure-Based Drug Repurposing Approach to Identify Potential CYP1B1 Inhibitors was written by Raju, Baddipadige;Narendra, Gera;Verma, Himanshu;Kumar, Manoj;Sapra, Bharti;Kaur, Gurleen;jain, Subheet Kumar;Silakari, Om. And the article was included in ACS Omega in 2022.SDS of cas: 10238-21-8 This article mentions the following:

Drug-metabolizing enzyme (DME)-mediated pharmacokinetic resistance of some clin. approved anticancer agents is one of the main reasons for cancer treatment failure. In particular, some commonly used anticancer medicines, including docetaxel, tamoxifen, imatinib, cisplatin, and paclitaxel, are inactivated by CYP1B1. Currently, no approved drugs are available to treat this CYP1B1-mediated inactivation, making the pharmaceutical industries strive to discover new anticancer agents. Because of the extreme complexity and high risk in drug discovery and development, it is worthwhile to come up with a drug repurposing strategy that may solve the resistance problem of existing chemotherapeutics. Therefore, in the current study, a drug repurposing strategy was implemented to find the possible CYP1B1 inhibitors using machine learning (ML) and structure-based virtual screening (SB-VS) approaches. Initially, three different ML models were developed such as support vector machines (SVMs), random forest (RF), and artificial neural network (ANN); subsequently, the best-selected ML model was employed for virtual screening of the selleckchem database to identify potential CYP1B1 inhibitors. The inhibition potency of the obtained hits was judged by analyzing the crucial active site amino acid interactions against CYP1B1. After a thorough assessment of docking scores, binding affinities, as well as binding modes, four compounds were selected and further subjected to in vitro anal. From the in vitro anal., it was observed that chlorprothixene, nadifloxacin, and ticagrelor showed promising inhibitory activity toward CYP1B1 in the IC₅₀ range of 0.07-3.00 μM. These new chem. scaffolds can be explored as adjuvant therapies to address CYP1B1-mediated drug-resistance problems. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8SDS of cas: 10238-21-8).

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.SDS of cas: 10238-21-8

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

Terminalia catappa aqueous leaf extract reverses insulin resistance, improves glucose transport and activates PI3K/AKT signalling in high fat/streptozotocin-induced diabetic rats was written by Iheagwam, Franklyn Nonso;Iheagwam, Olawumi Toyin;Onuoha, Michael Kemjika;Ogunlana, Olubanke Olujoke;Chinedu, Shalom Nwodo. And the article was included in Scientific Reports in 2022.Reference of 10238-21-8 This article mentions the following:

Rising prevalence of type 2 diabetes mellitus (T2DM) in sub-Saharan Africa has necessitated surveys of antidiabetic medicinal plants. This study assessed the antidiabetic mechanism of Terminalia catappa aqueous leaf extract (TCA) in high fat/low dose streptozotocin-induced type 2 diabetic rats. T2DM was induced by a combination of high-fat diet and low dose STZ (30 mg/kg bw) and the animals were administered with TCA (400 and 800 mg/kg bw) orally daily for 28 days. Biochem. parameters and indexes for diabetes including renal function tests and pancreatic histol. were evaluated. Relative expression of hepatic insulin resistance, signalling and glucose transport genes were also assessed. Induction of T2DM resulted in significant (p < 0.05) weight loss, dysregulated glucose level and clearance, electrolyte imbalance and disrupted diabetic biochem. parameters. Diabetes onset also perturbed β-cell function and insulin resistance indexes, damaged pancreas microanatomy, while disrupting the expression of insulin receptor substrate 1 (IRS-1), phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT) and glucose transporter isoform 4 (GLUT-4) mRNA. Oral treatment of diabetic animals with TCA significantly (p < 0.05) ameliorated alterations due to T2DM induction in a manner comparable with glibenclamide. These results suggest TCA exerts its antidiabetic action by reversing insulin resistance, improving glucose transport and activating PI3K/AKT signalling. 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. 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.Reference of 10238-21-8

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

Active and strippable PVA/Borax/NaBO₃ hydrogel for effective containment and decontamination of chemical warfare agents was written by Redy Keisar, Orit;Nahum, Victoria;Yehezkel, Lea;Marcovitch, Itzhak;Columbus, Ishay;Fridkin, Gil;Chen, Ravit. And the article was included in ACS Omega in 2021.Application In Synthesis of N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) This article mentions the following:

Active gels present unique potential for the decontamination of chem. warfare agents (CWAs) as they strongly adhere to surfaces, thus allowing prolonged decontamination time. Herein, we present a decontamination hydrogel based on polyvinyl alc./borax, which contains sodium perborate (NaBO₃), as an in situ source of the active ingredient hydrogen peroxide. Developed as a binary formulation, this gel instantly forms and effectively sticks when sprayed on various matrixes, including porous and vertically positioned matrixes. The gel efficiently detoxified the CWAs sarin (GB), O-Et S-2-(diisopropylamino)ethyl methylphosphonothioate (VX), and sulfur mustard (HD) in test tubes (2μL CWA/0.5 mL gel) to provide nontoxic products with reaction half-lives of <3, 45 and 113 min, resp. The gel was also shown to efficiently decontaminate surfaces contaminated with VX (5-7 mg, 8-12 mL of gel, i.e., >99%) and to prevent GB evaporation, as proven by laboratory wind tunnel experiments The universal decontamination abilities of this mild hydrogel, as well as its facile application and removal processes suggest that it holds high potential for future development as a new CWA decontamination tool. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Application In Synthesis of N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) 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 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.Application In Synthesis of N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)

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

Visible-Light-Promoted Carboimination of Unactivated Alkenes for the Synthesis of Densely Functionalized Pyrroline Derivatives was written by Cai, Sai-Hu;Xie, Jia-Hao;Song, Shengjin;Ye, Lu;Feng, Chao;Loh, Teck-Peng. And the article was included in ACS Catalysis in 2016.Quality Control of 4-Bromo-N-methoxy-N-methylbenzamide This article mentions the following:

An efficient strategy which integrates visible-light-induced iminyl-radical formation with carboimination of unactivated alkenes has been developed for the easy access of densely functionalized pyrroline derivatives With fac-[Ir(ppy)₃] as photoredox catalyst, the acyl oximes were converted into iminyl radical intermediates by one electron reduction, and evolve through a cascade of intramol. cyclization and intermol. carbon radical trapping to give the functionalized pyrrolines. The utilization of silyl enol ethers as coupling partners not only allows the introduction of synthetically useful ketone functionalities but also renders catalyst regeneration without any external reductants. This protocol is characterized by its mild reaction conditions and the tolerance of a broad range of functionalities. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2Quality Control of 4-Bromo-N-methoxy-N-methylbenzamide).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) 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 freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Quality Control of 4-Bromo-N-methoxy-N-methylbenzamide

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

Development of CDK2 and CDK5 Dual Degrader TMX-2172 was written by Teng, Mingxing;Jiang, Jie;He, Zhixiang;Kwiatkowski, Nicholas P.;Donovan, Katherine A.;Mills, Caitlin E.;Victor, Chiara;Hatcher, John M.;Fischer, Eric S.;Sorger, Peter K.;Zhang, Tinghu;Gray, Nathanael S.. And the article was included in Angewandte Chemie, International Edition in 2020.Name: 4-Amino-3-methylbenzenesulfonamide This article mentions the following:

Cyclin-dependent kinase 2 (CDK2) is a potential therapeutic target for the treatment of cancer. Development of CDK2 inhibitors has been extremely challenging as its ATP-binding site shares high similarity with CDK1, a related kinase whose inhibition causes toxic effects. Here, we report the development of TMX-2172(I), a heterobifunctional CDK2 degrader with degradation selectivity for CDK2 and CDK5 over not only CDK1, but transcriptional CDKs (CDK7 and CDK9) and cell cycle CDKs (CDK4 and CDK6) as well. In addition, we demonstrate that antiproliferative activity in ovarian cancer cells (OVCAR8) depends on CDK2 degradation and correlates with high expression of cyclin E1 (CCNE1), which functions as a regulatory subunit of CDK2. Collectively, our work provides evidence that TMX-2172 represents a lead for further development and that CDK2 degradation is a potentially valuable therapeutic strategy in ovarian and other cancers that overexpress CCNE1. In the experiment, the researchers used many compounds, for example, 4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4Name: 4-Amino-3-methylbenzenesulfonamide).

4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4) 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.Name: 4-Amino-3-methylbenzenesulfonamide

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

Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity was written by Buchstaller, Hans-Peter;Anlauf, Uwe;Dorsch, Dieter;Kuhn, Daniel;Lehmann, Martin;Leuthner, Birgitta;Musil, Djordje;Radtki, Daniela;Ritzert, Claudio;Rohdich, Felix;Schneider, Richard;Esdar, Christina. And the article was included in Journal of Medicinal Chemistry in 2019.Category: amides-buliding-blocks This article mentions the following:

Tankyrases 1 and 2 (TNKS1/2) are promising pharmacol. targets which recently gained interest for anticancer therapy in Wnt pathway dependent tumors. 2-Aryl-quinazolinones were identified and optimized into potent tankyrase inhibitors through SAR exploration around the quinazolinone core and the 4′-position of the Ph residue. These efforts were supported by anal. of TNKS X-ray and Watermap structures and resulted in compound 5k(I), a potent, selective tankyrase inhibitor with favorable pharmacokinetic properties. The X-ray structure of I in complex with TNKS1 was solved and confirmed the design hypothesis. Modulation of Wnt pathway activity was demonstrated with this compound in a colorectal xenograft model in vivo. In the experiment, the researchers used many compounds, for example, 6-Chloro-2-aminobenzamide (cas: 54166-95-9Category: amides-buliding-blocks).

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. 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.Category: amides-buliding-blocks

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

Research on low-temperature desizing-scouring-hydroperoxide-bleaching in one bath process for pure cotton fabric with biological enzyme was written by Xu, Yi;Gao, Bing-sheng. And the article was included in Ranzheng Jishu in 2015.Application In Synthesis of N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) This article mentions the following:

Typical amylase 2000L, cellulase CR and pectase L were optimized and the biocompatibility and synergistic effect were investigated. Process conditions of various enzymes mixtures and complex phosphoesterasum were discussed to obtain optimized process of complex phosphoesterasum in desizing and scouring treatments. Desizing, scouring and bleaching production process in one bath was realized by combining biol. enzyme compound technol. with low temperature oxygen bleaching process. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Application In Synthesis of N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)).

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. 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 N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)

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