Category: 683-57-8

In 2022,Wang, Yaqian; Liu, Huihui; Yang, Xianhai; Wang, Lianjun published an article in Science of the Total Environment. The title of the article was 《Aquatic toxicity and aquatic ecological risk assessment of wastewater-derived halogenated phenolic disinfection byproducts》.Related Products of 683-57-8 The author mentioned the following in the article:

Increasing number of wastewater-derived aliphatic and phenolic disinfection byproducts (DBPs) were discharged into aquatic environment with the discharge of disinfected wastewater. However, the currently available aquatic toxicity data and the aquatic ecol. risk information of them are limited, especially for wastewater-derived phenolic DBPs. In this study, we investigated the acute toxicity of 7 phenolic DBPs that selected from the typical five groups of phenolic DBPs (2,4,6-trihalo-phenols, 2,6-dihalo-4-nitrophenols, 3,5-dihalo-4-hydroxybenzaldehydes, 3,5-dihalo-4-hydroxybenzoic acids and halo-salicylic acids) and 4 aliphatic DBPs to Gobiocypris rarus and also assessed their potential aquatic ecol. risk. Exptl. results indicated that the half lethal concentration (LC50) values of 2,4,6-trihalo-phenols and 2,6-dihalo-4-nitrophenols ranged from 1 to 10 mg/L; While that of 3,5-dihalo-4-hydroxybenzaldehydes was between 10 and 100 mg/L, and 3,5-dihalo-4-hydroxybenzoic acids and halo-salicylic acids was >100 mg/L. The toxicity mode of action (MOA) identification results from three methods suggested that no clear and consistent MOA were obtained for those 11 DBPs currently. The species-specific aquatic toxicity anal. results highlighted that no aquatic species would be considered as the most sensitive species for all 11 DBPs. However, crustacean and fish were more sensitive than that of algae for most of tested compounds Lastly, the aquatic ecol. risk assessment results of those 11 DBPs revealed that all 7 phenolic and 2 aliphatic DBPs (2-bromoacetamide and bromodichloromethane) had low aquatic ecol. risk, while dichloroacetic acid and dibromoacetonitrile had high aquatic ecol. risk. The low environmental concentration was the main reason why high toxic phenolic DBPs (2,4,6-trihalo-phenols and 2,6-dihalo-4-nitrophenols) exhibited low ecol. risk. Their ecol. risk may increase with the increases of corresponding environmental concentration Thus, more efforts should be made to determine other potential harmful effects of those high toxic phenolic DBPs and to minimize their potential ecol. risk by taking appropriate measures. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8Related Products of 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Related Products of 683-57-8

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

Avadhani, Anusha; Iniyavan, Pethaperumal; Kumar, Yogendra; Ila, Hiriyakkanavar published their research in Journal of Organic Chemistry in 2021. The article was titled 《Single-Pot Preparation of 4-Amino-2-(het)aryl-5-Substituted Thiazoles Employing Functionalized Dithioesters as Thiocarbonyl Precursors》.Name: 2-Bromoacetamide The article contains the following contents:

An effective, diversity oriented, one-pot reaction of 4-amino-2-(het)aryl/alkyl-5-functionalized thiazoles was disclosed, utilizing aryl/heteroaryl/alkyl dithioesters as thiocarbonyl coupling partners in a modified Thorpe-Ziegler type cyclization. The reaction proceeds at room temperature, under mild conditions, in excellent yields, displayed broad functional group compatibility at 2 and 5 positions of thiazoles. This synthetic strategy was further expanded for the one-pot construction of two highly potent tubulin polymerization inhibitors, i.e., 2-(het)aryl-4-amino-5-(3,4,5-trimethoxyaroyl) thiazoles, in high yields. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Name: 2-Bromoacetamide)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Name: 2-Bromoacetamide

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

《Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects》 was written by Pflimlin, Elsa; Zhou, Zhihong; Amso, Zaid; Fu, Qiangwei; Lee, Candy; Muppiddi, Avinash; Joseph, Sean B.; Nguyen-Tran, Van; Shen, Weijun. HPLC of Formula: 683-57-8 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

The effects of oxytocin on food intake and body weight reduction have been demonstrated in both animal models and human clin. studies. Despite being efficacious, oxytocin is enzymically unstable and thus considered to be unsuitable for long-term use in patients with obesity. Herein, a series of oxytocin derivatives were engineered through conjugation with fatty acid moieties that are known to exhibit high binding affinities to serum albumin. One analog (OT-12) in particular was shown to be a potent full agonist at the oxytocin receptor (OTR) in vitro with good selectivity and long half-life (24 h) in mice. Furthermore, OT-12 is peripherally restricted, with very limited brain exposure (1/190 of the plasma level). In a diet-induced obesity mouse model, daily s.c. administration of OT-12 exhibited more potent anorexigenic and body weight reducing effects than carbetocin. Thus, our results suggest that the long-acting, peripherally restricted OTR agonist may offer potential therapeutic benefits for obesity. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8HPLC of Formula: 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.HPLC of Formula: 683-57-8

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

In 2019,Science of the Total Environment included an article by Ding, Xinliang; Zhu, Jingying; Wang, Xiaoxiao; Zhou, Weijie; Wu, Keqin; Zhou, Zhu; Zhou, Kun; Wu, Di; Jiao, Jiandong; Xia, Yankai; Wang, Xinru. SDS of cas: 683-57-8. The article was titled 《Different cytotoxicity of disinfection by-product haloacetamides on two exposure pathway-related cell lines: Human gastric epithelial cell line GES-1 and immortalized human keratinocyte cell line HaCaT》. The information in the text is summarized as follows:

Humans are exposed to disinfection byproducts (DBPs) mainly through drinking water ingestion and dermal contact. As an emerging class of nitrogenous DBPs (N-DBPs), haloacetamides (HAcAms) have been found to have significantly higher cytotoxicity than regulated DBPs. In this study, we investigated the cytotoxicity of HAcAms on two exposure pathway-related cell lines: human gastric epithelial GES-1 cells and immortalized keratinocytes HaCaT. Our results showed that the ranking order of cytotoxicity of 13 HAcAms was different between HaCaT and GES-1 cells. In addition, the 50% inhibitive concentration in HaCaT was 1.01-3.29 times that in GES-1. Further comparison among GES-1, HaCaT and CHO cell lines confirmed that different cell lines exhibited different sensitivity to the same compound Importantly, HAcAms showed 5.83-7.13 × 104 times higher toxicity than the well-clarified DBP chloroform, clearly demonstrating the increased toxicity of HAcAms. Finally, using a novel high-content screening (HCS) anal., we found that 39.29% of chlorinated HAcAms, 42.86% of brominated HAcAms and 16.07% of iodinated HAcAms significantly affected at least one of the cell-health parameters, such as nuclear size, membrane permeability, mitochondrial membrane potential, or cytochrome c release, in GES-1 or HaCaT cells. Thus, brominated HAcAms appear to have stronger effects under the sublethal exposure dose, possibly causing cytotoxicity via apoptosis. Together, our study provides new insights to the toxicity of HAcAms and a comprehensive toxicol. dataset for health risk assessment. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8SDS of cas: 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.SDS of cas: 683-57-8

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

Mouchel Dit Leguerrier, D.; Barre, R.; Ruet, Q.; Imbert, D.; Philouze, C.; Fries, P. H.; Martel-Frachet, V.; Molloy, J. K.; Thomas, F. published their research in Dalton Transactions in 2021. The article was titled 《Lanthanide complexes of DOTA-nitroxide conjugates for redox imaging: spectroelectrochemistry, CEST, relaxivity, and cytotoxicity》.Synthetic Route of C2H4BrNO The article contains the following contents:

The lanthanide(III) complexes (Gd, Eu, Dy, and Yb) of DOTA tris(amide) and bis(amide) derivatives (L1 and L2) featuring one redox active TEMPO arm were prepared Ligand L2 harbours an alkyne fragment for further functionalization. The x-ray crystal structure of ligand L2 in complexation with Na+ was solved. The complexes showed in their CV one oxidation wave (0.26-0. 34 V vs. Fc+/Fc) due to an oxoammonium/nitroxide redox couple and a broad reduction corresponding to the nitroxide/hydroxylamine system. The Eu complexes demonstrated the presence of one water mol. in their coordination sphere. The nitroxide complexes were characterized by EPR spectroscopy, showing the typical 3-line pattern in the high temperature regime, which is quenched upon the addition of ascorbate (reduction into hydroxylamine). In their nitroxide form, the complexes show essentially no CEST peak. Conversely, the reduced complexes demonstrate a 12% CEST peak at 51 ppm, corresponding to the metal bound water mol. Fast exchange precluded the CEST activity for the amide protons. All the complexes proved to be essentially non-toxic for M21 cells at concentrations up to 50μM. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8Synthetic Route of C2H4BrNO)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Synthetic Route of C2H4BrNO

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

《Ammonia-Mediated Bromate Inhibition during Ozonation Promotes the Toxicity Due to Organic Byproduct Transformation》 was published in Environmental Science & Technology in 2020. These research results belong to Wu, Qian-Yuan; Yang, Lu-Lin; Zhang, Xin-Yang; Wang, Wen-Long; Lu, Yao; Du, Ye; Lu, Yun; Hu, Hong-Ying. Recommanded Product: 2-Bromoacetamide The article mentions the following:

Ammonia (NH4+) and hydrogen peroxide (H2O2) have been widely used to inhibit bromate formation during ozonization. However, organic byproducts can also pose a risk under these conditions. During bromate inhibition, the influence of NH4+ and H2O2 on organic byproducts and their toxicity should be elucidated. Our study found that NH4+ suppressed organic bromine, but might result in increased toxicity. Adding 0.5 mg/L of NH4+-N substantially increased both the formation of cytotoxicity and genotoxicity (DNA double-strand breaks) of organic byproducts from 0.6 to 1.6 mg-phenol/L, and from 0.3 to 0.8μg-4-NQO/L (0.5 mg/L Br-, 5 mg/L O3). NH4+ decreased bromate, but increased the overall toxicity of the integrated byproducts (organic byproducts and bromate). Organic nitrogen measurements and 15N isotope anal. showed enhanced incorporation of nitrogen into organic matter when NH4+ and Br- coexisted during ozonization. NH4+ decreased the formation of brominated acetonitriles, but enhanced the formation of brominated nitromethanes and brominated acetamides. These brominated nitrogenous byproducts were partially responsible for this increase in toxicity. Different from ammonia, H2O2 could reduce both bromate and the toxicity of organic byproducts. In the presence of 0.5 mg/L Br- and 10 mg/L O3, adding H2O2 (0.5 mM) substantially suppressed bromate, cytotoxicity formation and genotoxicity formation by 88%, 63% and 67%. This study highlights that focusing on bromate control with NH4+ addition might result in higher toxicity. Efforts are needed to effectively control the toxicities of bromate and organic byproducts simultaneously. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8Recommanded Product: 2-Bromoacetamide)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Recommanded Product: 2-Bromoacetamide

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

In 2019,Bioorganic & Medicinal Chemistry included an article by de Heuvel, Erik; Singh, Abhimanyu K.; Edink, Ewald; van der Meer, Tiffany; van der Woude, Melanie; Sadek, Payman; Krell-Joergensen, Mikkel P.; van den Bergh, Toine; Veerman, Johan; Caljon, Guy; Kalejaiye, Titilola D.; Wijtmans, Maikel; Maes, Louis; de Koning, Harry P.; Jan Sterk, Geert; Siderius, Marco; de Esch, Iwan J. P.; Brown, David G.; Leurs, Rob. Application In Synthesis of 2-Bromoacetamide. The article was titled 《Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors》. The information in the text is summarized as follows:

Several 3′,5′-cyclic nucleotide phosphodiesterases (PDEs) have been validated as good drug targets for a large variety of diseases. Trypanosoma brucei PDEB1 (TbrPDEB1) has been designated as a promising drug target for the treatment of human African trypanosomiasis. Recently, the first class of selective nanomolar TbrPDEB1 inhibitors was obtained by targeting the parasite specific P-pocket. However, these biphenyl-substituted tetrahydrophthalazinone-based inhibitors did not show potent cellular activity against Trypanosoma brucei (T. brucei) parasites, leaving room for further optimization. Herein, we report the discovery of a new class of potent TbrPDEB1 inhibitors that display improved activities against T. brucei parasites. Exploring different linkers between the reported tetrahydrophthalazinone core scaffold and the amide tail group resulted in the discovery of alkynamide phthalazinones as new TbrPDEB1 inhibitors, which exhibit submicromolar activities vs. T. brucei parasites and no cytotoxicity to human MRC-5 cells. Elucidation of the crystal structure of alkynamide 8b (NPD-048) bound to the catalytic domain of TbrPDEB1 shows a bidentate interaction with the key-residue Gln874 and good directionality towards the P-pocket. Incubation of trypanosomes with alkynamide 8b results in an increase of intracellular cAMP, validating a PDE-mediated effect in vitro and providing a new interesting compound series for further studies towards selective TbrPDEB1 inhibitors with potent phenotypic activity. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8Application In Synthesis of 2-Bromoacetamide)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Application In Synthesis of 2-Bromoacetamide

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

《Discovery of CyclicBoronic Acid QPX7728, an Ultrabroad-SpectrumInhibitor of Serine and Metallo-β-lactamases》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Hecker, Scott J.; Reddy, K. Raja; Lomovskaya, Olga; Griffith, David C.; Rubio-Aparicio, Debora; Nelson, Kirk; Tsivkovski, Ruslan; Sun, Dongxu; Sabet, Mojgan; Tarazi, Ziad; Parkinson, Jonathan; Totrov, Maxim; Boyer, Serge H.; Glinka, Tomasz W.; Pemberton, Orville A.; Chen, Yu; Dudley, Michael N.. Related Products of 683-57-8 The article mentions the following:

Despite major advances in the beta-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among these are the Class B (metallo) enzyme NDM-1 of Enterobacteriaceae and the Class D (OXA) enzymes of Acinetobacter baumannii. Continuing the boronic acid program that led to vaborbactam, efforts were directed toward expanding the spectrum to allow treatment of a wider range of organisms. Through key structural modifications of a bicyclic lead, stepwise gains in spectrum of inhibition were achieved, ultimately resulting in QPX7728, I. This compound displays a remarkably broad spectrum of inhibition, including Class B and Class D enzymes, and is little affected by porin modifications and efflux. I is a promising agent for use in combination with a beta-lactam antibiotic for the treatment of a wide range of multidrug resistant gram-neg. bacterial infections, by both i.v. and oral administration. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Related Products of 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Related Products of 683-57-8

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

HPLC of Formula: 683-57-8In 2021 ,《Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds》 was published in Journal of Medicinal Chemistry. The article was written by Pallesen, Jakob S.; Narayanan, Dilip; Tran, Kim T.; Solbak, Sara M. Oe.; Marseglia, Giuseppe; Soerensen, Louis M. E.; Hoej, Lars J.; Munafo, Federico; Carmona, Rosa M. C.; Garcia, Anthony D.; Desu, Haritha L.; Brambilla, Roberta; Johansen, Tommy N.; Popowicz, Grzegorz M.; Sattler, Michael; Gajhede, Michael; Bach, Anders. The article contains the following contents:

Targeting the protein-protein interaction (PPI) between nuclear factor erythroid 2-related factor 2 (Nrf2) and Kelch-like ECH-associated protein 1 (Keap1) is a potential therapeutic strategy to control diseases involving oxidative stress. Here, six classes of known small-mol. Keap1-Nrf2 PPI inhibitors were dissected into 77 fragments in a fragment-based deconstruction reconstruction (FBDR) study and tested in four orthogonal assays. This gave 17 fragment hits of which six were shown by X-ray crystallog. to bind in the Keap1 Kelch binding pocket. Two hits were merged into pyrazole I with a 220-380-fold stronger affinity (Ki = 16μM) relative to the parent fragments. Systematic optimization resulted in several novel analogs with Ki values of 0.04-0.5μM, binding modes determined by X-ray crystallog., and enhanced microsomal stability. This demonstrates how FBDR can be used to find new fragment hits, elucidate important ligand-protein interactions, and identify new potent inhibitors of the Keap1-Nrf2 PPI. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8HPLC of Formula: 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.HPLC of Formula: 683-57-8

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

Application of 683-57-8In 2022 ,《Bis(amido)bis(oxinate)diamine Ligands for theranostic radiometals》 appeared in Journal of Inorganic Biochemistry. The author of the article were Southcott, Lily; Whetter, Jennifer N.; Wharton, Luke; Patrick, Brian O.; Zarschler, Kristof; Kubeil, Manja; Stephan, Holger; Jaraquemada-Pelaez, Maria de Guadalupe; Orvig, Chris. The article conveys some information:

With the interest in radiometal-containing diagnostic and therapeutic pharmaceuticals increasing rapidly, appropriate ligands to coordinate completely and stably said radiometals is essential. Reported here are two novel, bis(amido)bis(oxinate)diamine ligands, H2amidohox (2,2′-(ethane-1,2-diylbis(((8-hydroxyquinolin-2-yl)methyl)azanediyl))diacetamide) and H2amidoC3hox (2,2′-(propane-1,3-diylbis(((8-hydroxyquinolin-2-yl)methyl)azanediyl))diacetamide), that combine two 8-hydroxyquinoline and amide donor groups and differ by one carbon in their 1,2-ethylenediamine vs. 1,3-diaminopropane backbones, resp. Both ligands were thoroughly studied via metal complexation, solution thermodn. and radiolabeling with three radiometal ions: [nat/64Cu]Cu2+, [nat/111In]In3+, and [nat/203Pb]Pb2+. X-ray crystallog. determined the structures of the hexacoordinated Cu2+-ligand complexes, indicating a better fit of Cu2+ to the H2amidohox binding pocket. Concentration dependent radiolabeling with [64Cu]Cu2+ was successfully quant. as low as 1μM with H2amidohox and 10μM with H2amidoC3hox within 5 min at room temperature However, [64Cu][Cu(amidohox)] maintained higher kinetic inertness against a superoxide dismutase enzyme-challenge assay and ligand challenges compared to the [64Cu][Cu(amidoC3hox)] counterpart. Similarly, H2amidohox had significantly higher radiochem. conversion with both [111In]In3+ (97% at 1μM) and [203Pb]Pb2+ (97% at 100μM) under mild conditions compared to H2amidoC3hox (76% with [111In]In3+ at 1μM and 0% with [203Pb]Pb2+). By studying non-radioactive and radioactive complexation with both ligands, a comprehensive understanding of the coordination differences between two- and three-carbon diamine backbones is discussed. Overall, the ethylenediamine backbone of H2amidohox proves to be superior in rapid, mild radiolabeling and kinetic inertness towards competing ligands and proteins. After reading the article, we found that the author used 2-Bromoacetamide(cas: 683-57-8Application of 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Application of 683-57-8

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