Category: amides-buliding-blocks

Collection of ion-trap mass spectra of sulfonylurea pyrolysis products was written by Galletti, Guido C.;Dinelli, Giovanni;Chiavari, Giuseppe. And the article was included in Journal of Mass Spectrometry in 1995.Synthetic Route of C8H10ClNO3S This article mentions the following:

The pyrograms of 14 sulfonylureas, i.e. herbicides characterized by high biol. activity and low application dose are discussed and the mass spectra of over 30 relevant pyrolysis products as obtained with a heated filament pyrolyzer interfaces to a capillary gas chromatograph/ion-trap detector mass spectrometer are presented. Such a data compilation is useful for diagnostic purposes for both intact sulfonylureas and their metabolites after determination in soil, because metabolites and pyrolysis products are often identical and most of their mass spectra are lacking in com. available mass spectral libraries. The performance of the ion-trap detector based on the quality of the mass spectra is briefly discussed. In the experiment, the researchers used many compounds, for example, 2-(2-Chloroethoxy)benzenesulfonamide (cas: 82097-01-6Synthetic Route of C8H10ClNO3S).

2-(2-Chloroethoxy)benzenesulfonamide (cas: 82097-01-6) 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. 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.Synthetic Route of C8H10ClNO3S

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

Efficient and Targeted Suppression of Human Lung Tumor Xenografts in Mice with Methotrexate Sodium Encapsulated in All-Function-in-One Chimeric Polymersomes was written by Yang, Weijing;Zou, Yan;Meng, Fenghua;Zhang, Jian;Cheng, Ru;Deng, Chao;Zhong, Zhiyuan. And the article was included in Advanced Materials (Weinheim, Germany) in 2016.Related Products of 7413-34-5 This article mentions the following:

We have demonstrated that anisamide-functionalizeddisulfide-crosslinked chimeric polymersomes can efficiently load and selectively deliver and release MTX·2Na into sigma receptor-overexpressing H460 non-small lung cancer cell xenografts in vivo, leading to markedly improved tumor growth inhibition and survival rate as compared to the nontargeting polymersomes and com. Trexall controls. To the best of our knowledge, this represents the first report on efficient tumor-targeting delivery of MTX·2Na using polymersomes. These disulfide-crosslinked chimeric polymersomes possess several extraordinary features over previously reported nanosystems including high MTX·2Na loading, superior in vivo stability,enhanced accumulation in tumors, selective and efficient uptake by tumor cells, fast intracellular release of MTX·2Na and low side effects, which render them an “all-function-in-one”nanoplatform for safe and potent cancer chemotherapy. 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: 7413-34-5Related Products of 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.Related Products of 7413-34-5

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

Establishment of an effective activated peroxide system for low-temperature cotton bleaching using synthesized tetramido macrocyclic iron complex was written by Yu, Deyou;Wu, Minghua;Lin, Junxiong. And the article was included in Fibers and Polymers in 2017.Application of 10543-57-4 This article mentions the following:

In this study, the tetramido macrocyclic iron complex (Fe-TAML) was successfully synthesized, and then it was characterized using ¹H NMR, electrospray ionization mass spectrometry (EIS-MS) and elemental anal. An activated peroxide system was established for low-temperature bleaching of cotton by combining the synthesized catalyst (Fe-TAML) with hydrogen peroxide. Exptl. results showed that the Fe-TAML/H₂O₂ bleaching system exhibited effective bleaching performance in the use of 2 μM Fe-TAML, 20 g/l H₂O₂, 1 g/l NaHCO₃, 2 g/l scouring agent and 2 g/l wetting agent at 60 °C for 60 min. In comparison with the conventional bleaching system, the Fe-TAML/H₂O₂ system provided bleached cotton with a superior degree of whiteness, higher tensile strength and acceptable water absorbency. The application of Fe-TAML was expanded and the activated peroxide system may provide a green approach for the cotton bleaching. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Application of 10543-57-4).

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 can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Application of 10543-57-4

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

Evaluation of cationic channel TRPV2 as a novel biomarker and therapeutic target in Leukemia-Implications concerning the resolution of pulmonary inflammation was written by Siveen, Kodappully S.;Prabhu, Kirti S.;Parray, Aeijaz S.;Merhi, Maysaloun;Arredouani, Abdelilah;Chikri, Mohamed;Uddin, Shahab;Dermime, Said;Mohammad, Ramzi M.;Steinhoff, Martin;Janahi, Ibrahim A.;Azizi, Fouad. And the article was included in Scientific Reports in 2019.Application of 53902-12-8 This article mentions the following:

Patients treated during leukemia face the risk of complications including pulmonary dysfunction that may result from infiltration of leukemic blast cells (LBCs) into lung parenchyma and interstitium. In LBCs, we demonstrated that transient receptor potential vanilloid type 2 channel (TRPV2), reputed for its role in inflammatory processes, exhibited oncogenic activity associated with alteration of its mol. expression profile. TRPV2 was overexpressed in LBCs compared to normal human peripheral blood mononuclear cells (PBMCs). Addnl., functional full length isoform and nonfunctional short form pore-less variant of TRPV2 protein were up-regulated and down-regulated resp. in LBCs. However, the opposite was found in PBMCs. TRPV2 silencing or pharmacol. targeting by Tranilast (TL) or SKF96365 (SKF) triggered caspace-mediated apoptosis and cell cycle arrest. TL and SKF inhibited chemotactic peptide fMLP-induced response linked to TRPV2 Ca²⁺ activity, and down-regulated expression of surface marker CD38 involved in leukemia and lung airway inflammation. Challenging lung airway epithelial cells (AECs) with LBCs decreased (by more than 50%) transepithelial resistance (TER) denoting barrier function alteration. Importantly, TL prevented such loss in TER. Therefore, TRPV2 merits further exploration as a pharmacodynamic biomarker for leukemia patients (with pulmonary inflammation) who might be suitable for a novel [adjuvant] therapeutic strategy based on TL. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Application of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. 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.Application of 53902-12-8

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

Hydrophobic Pockets of HPMC Enable Extremely Short Reaction Times in Water was written by Petkova, Desislava;Borlinghaus, Niginia;Sharma, Sudripet;Kaschel, Johannes;Lindner, Tanja;Klee, Johanna;Jolit, Anais;Haller, Vanessa;Heitz, Stephanie;Britze, Katarina;Dietrich, Justin;Braje, Wilfried M.;Handa, Sachin. And the article was included in ACS Sustainable Chemistry & Engineering in 2020.COA of Formula: C9H10BrNO2 This article mentions the following:

A methodol. for formation of ligated ultrasmall in-situ generated Pd nanoparticles in the hydrophobic pockets of benign cellulose derivative hydroxypropyl methylcellulose (HPMC) for chem. reactions to proceed very fast in water under mild reaction conditions was reported. Unprecedented short reaction times were exemplified for the Buchwald-Hartwig amination reaction of aryl bromides and aryl amines using in-situ generated Pd nanoparticles in aqueous HMPC solution to afford substituted aryl amines RNHR¹ [R = 1-naphthyl, 3-MeC₆H₄, 2-MeOC₆H₄, etc.; R¹ = Ph, 4-MeC₆H₄, 1-naphthyl, etc.]. In addition, very short reaction times were also demonstrated for the peptide coupling of carboxylic acids and amines using in-situ generated Pd nanoparticles in aqueous HMPC solution to afford aryl amides R²C(O)NR³R⁴ [R² = Bn, 4-ClC₆H₄, 4-BrC₆H₄, etc.; R³ = OMe, n-hexyl, 3,5-(Me)₂C₆H₃, etc.; R⁴ = H, Me, etc.]. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2COA of Formula: C9H10BrNO2).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. 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.COA of Formula: C9H10BrNO2

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

Anti-cancer effects of Tranilast: An update was written by Osman, Soha;Raza, Afsheen;Al-Zaidan, Lobna;Inchakalody, Varghese Philipose;Merhi, Maysaloun;Prabhu, Kirti S.;Abdelaziz, Nouha;Hydrose, Shereena;Uddin, Shahab;Dermime, Said. And the article was included in Biomedicine & Pharmacotherapy in 2021.Computed Properties of C18H17NO5 This article mentions the following:

Tranilast (TRN) or (N-3,4-dimethoxy cinnamoyl-anthranilic acid) is an analog of a tryptophan metabolite and is identified mainly as an anti-allergic agent with limited side effects. The anti-cancer effects of tranilast either alone or in combination with chemotherapeutic drugs have been evidenced in several pre-clin. studies. The main mechanism of action of tranilast includes targeting and modulation of various signaling and immune regulatory pathways including Transforming growth factor-beta (TGF-β), nuclear factor kappa-light-chainenhancer of activated B cells (NF-κB), phosphatidylinositol 3-kinase (PI3K), MAP-Kinase (MAPK), Protein kinase B (Akt/PKB), c-Jun N-terminal kinase, modulation of cancer stem cells, etc. Most of these pathways are involved in tumor proliferation, invasion, and metastasis and it is postulated that tranilast, with its low toxicity profile and high anti-carcinogenic abilities, can serve as a potential anti-tumorigenic agent. The main aim of this review is to provide updated information on the anti-cancer effects of tranilast and its significance as a therapeutic agent. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Computed Properties of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. 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.Computed Properties of C18H17NO5

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

NLRP3 inflammasome inhibitor ameliorates ischemic stroke by reprogramming the phenotype of microglia/macrophage in a murine model of distal middle cerebral artery occlusion was written by Jia, Hongning;Qi, Xiaoyuan;Fu, Lan;Wu, Huijun;Shang, Jinxing;Qu, Mingwei;Yang, Chaoping;Wang, Jianping. And the article was included in Neuropathology in 2022.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Stroke is one of the leading causes of death and disability worldwide. NLRP3 inflammasome has an essential role in the neuropathol. of stroke. Recent studies report that shifting the microglial M1 phenotype to the M2 phenotype protects against ischemic stroke. In the present study, the precise effects of Tranilast, a NLPR3 inflammasome inhibitor, on stroke were evaluated. We established a murine model of distal middle cerebral artery occlusion (dMCAO) and administered Tranilast to dMCAO-induced stroke mice. The NLRP3 level, caspase 1 activity, and infarct volume stroke mice were measured. The sensorimotor function, pro-inflammatory cytokine production, and M1/M2 marker expression were measured. The M1 phenotype was induced by treatment of BV2 microglia with lipopolysacharide and interferon γ, and these BV-2 cells were further treated with Tranilast. The expression of CD16 and CD206 was monitored. dMCAO increased the NLRP3 expression and enhanced caspase 1 activity. Tranilast treatment significantly decreased the infarct volume, improved sensorimotor function, and suppressed the production of inflammatory cytokines in stroke mice. Moreover, Tranilast decreased the M1 marker level while promoting the expression of M2 markers. In summary, our findings suggest that Tranilast ameliorates ischemic stroke through stimulating M2 polarization of microglia. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. 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.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Hemin-catalyzed biomimetic oxidative phenol-indole [3 + 2] reactions in aqueous media was written by Fu, Yu;Yu, Qile;Zhang, Yulong;Gao, Zhonghong;Wu, Yuzhou;Zhong, Fangrui. And the article was included in Organic & Biomolecular Chemistry in 2019.Reference of 1146-43-6 This article mentions the following:

A hemin/H₂O₂ catalytic system for oxidative phenol-indole [3 + 2] coupling in aqueous solution was developed, enabling benign synthesis of valuable benzofuroindolines under sustainable conditions. Mechanistic studies revealed the dual role of iron porphyrin responsible for both phenol oxidation and Lewis acid activation, which differs from the well-explored chem. of hemin in carbene and nitrene insertion reactions. A preliminary experiment with cytochrome c showed that the turnover of iron porphyrin was amenable for a macromol. setting with remarkable efficiency (∼13,300 TON). In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6Reference of 1146-43-6).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) 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.Reference of 1146-43-6

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

Evaluation of Suppressive Effects of Tranilast on the Invasion/Metastasis Mechanism in a Murine Pancreatic Cancer Cell Line was written by Kaneda, Munehisa;Obara, Hideaki;Suzuki, Keiichi;Takeuchi, Osamu;Takizawa, Asako;Osaku, Masayoshi;Matsubara, Hajime;Kitagawa, Yuko. And the article was included in Pancreas (Philadelphia, PA, United States) in 2017.Application of 53902-12-8 This article mentions the following:

Objectives: Numerous studies have investigated the mechanism of the antitumor effect of tranilast, well known as an antiallergic drug. Herein, we investigated the mechanism of the antitumor effects of tranilast using murine PAN 02 cell line. Methods: In an allograft mouse model, the number of metastatic sites in the liver was counted. Wound healing and chemoinvasion assay were performed to evaluate migration and invasive ability of PAN 02, resp. Activities of matrix metalloproteinases (MMPs) were evaluated by gelatin zymog. The expression of cofactors in the activation of MMP-2 was assessed by immunohistochem. staining at the front of metastasis. Results: The number of metastatic sites was reduced in tranilast-treated groups. Migration ability and tumor invasiveness were significantly inhibited by tranilast in a dose-dependent manner. Gelatin zymog. revealed inhibition of MMP-2 activity. Immunohistochem. staining showed remarkable attenuation of tissue inhibitor of metalloproteinase (TIMP-) 2 expression in tranilast-treated groups. Conclusions: Tissue inhibitor of metalloproteinase 2 is necessary for MMP-2 activation with interaction between membrane type 1-MMP and proMMP-2. These results suggested that tranilast may inhibit MMP-2 activation through attenuating TIMP-2 expression, resulting in inhibition of tumor invasion and metastasis. Our results showed possibility of tranilast in clin. application for novel cancer therapy. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Application of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. 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 of 53902-12-8

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

Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets was written by Mayhoub, Abdelrahman S.;Marler, Laura;Kondratyuk, Tamara P.;Park, Eun-Jung;Pezzuto, John M.;Cushman, Mark. And the article was included in Bioorganic & Medicinal Chemistry in 2012.Reference of 2670-38-4 This article mentions the following:

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biol. targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1). In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Reference of 2670-38-4).

3,4-Dichlorobenzamide (cas: 2670-38-4) 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 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.Reference of 2670-38-4

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