Category: 626-40-4

In 2017,Greulich, Tobias W.; Yamaguchi, Eriko; Doerenkamp, Carsten; Luebbesmeyer, Maximilian; Daniliuc, Constantin G.; Fukazawa, Aiko; Eckert, Hellmut; Yamaguchi, Shigehiro; Studer, Armido published 《Synthesis and Physical Properties of Strained Doubly Phosphorus-Bridged Biaryls and Viologens》.Chemistry – A European Journal published the findings.Electric Literature of C6H5Br2N The information in the text is summarized as follows:

New P/N-containing π-electron systems comprising fully planar biaryl arrays are synthesized by multiple radical phosphanylation. The biaryl moiety in these highly strained planar π-systems is rigidified by double P-bridging. The electronic properties of the core biaryl entity are varied by introducing N-donor substituents or by installing N-atoms within the π-system, thereby moving to the viologen core structure. The electrochem. and photophys. properties of these compounds are discussed and compared with those of related systems.3,5-Dibromoaniline(cas: 626-40-4Electric Literature of C6H5Br2N) was used in this study.

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Electric Literature of C6H5Br2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer’s disease》 were Srivastava, Pavan; Tripathi, Prabhash Nath; Sharma, Piyoosh; Shrivastava, Sushant Kumar. And the article was published in Bioorganic & Medicinal Chemistry in 2019. Electric Literature of C6H5Br2N The author mentioned the following in the article:

Novel hybrids N-(4-phenoxybenzyl)aniline were designed, synthesized, and evaluated for their potential AChE inhibitory activity along with antioxidant potential. The inhibitory potential (IC50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman’s method. Among all the tested compounds, 42 with trimethoxybenzene substituent showed maximum hAChE inhibition with the competitive type of enzyme inhibition (IC50 = 1.32 μM; Ki = 0.879 μM). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed favorable BBB permeability by most of the synthesized compounds Meanwhile, compound 42 also inhibited AChE-induced Aβ aggregation (39.5-66.9%) in thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 42. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 42 in brain homogenates. In the experiment, the researchers used 3,5-Dibromoaniline(cas: 626-40-4Electric Literature of C6H5Br2N)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Electric Literature of C6H5Br2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Related Products of 626-40-4In 2020 ,《Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity in Vivo Mouse Model》 appeared in Journal of Medicinal Chemistry. The author of the article were Fromont, Christophe; Atzori, Alessio; Kaur, Divneet; Hashmi, Lubna; Greco, Graziella; Cabanillas, Alejandro; Nguyen, Huy Van; Jones, D. Heulyn; Garzon, Miguel; Varela, Ana; Stevenson, Brett; Iacobini, Greg P.; Lenoir, Marc; Rajesh, Sundaresan; Box, Clare; Kumar, Jitendra; Grant, Paige; Novitskaya, Vera; Morgan, Juliet; Sorrell, Fiona J.; Redondo, Clara; Kramer, Andreas; Harris, C. John; Leighton, Brendan; Vickers, Steven P.; Cheetham, Sharon C.; Kenyon, Colin; Grabowska, Anna M.; Overduin, Michael; Berditchevski, Fedor; Weston, Chris J.; Knapp, Stefan; Fischer, Peter M.; Butterworth, Sam. The article conveys some information:

Polymorphisms in the region of the calmodulin-dependent kinase isoform D (CaMK1D) gene are associated with increased incidence of diabetes, with the most common polymorphism resulting in increased recognition by transcription factors and increased protein expression. While reducing CaMK1D expression has a potentially beneficial effect on glucose processing in human hepatocytes, there are no known selective inhibitors of CaMK1 kinases that can be used to validate or translate these findings. Here we describe the development of a series of potent, selective, and drug-like CaMK1 inhibitors that are able to provide significant free target cover in mouse models and are therefore useful as in vivo tool compounds Our results show that a lead compound from this series improves insulin sensitivity and glucose control in the diet-induced obesity mouse model after both acute and chronic administration, providing the first in vivo validation of CaMK1D as a target for diabetes therapeutics. The experimental process involved the reaction of 3,5-Dibromoaniline(cas: 626-40-4Related Products of 626-40-4)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Related Products of 626-40-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Andrews, David M.; Cartic, Sharon; Cosulich, Sabina; Divecha, Nullin; Faulder, Paul; Flemington, Vikki; Kern, Oliver; Kettle, Jason G.; MacDonald, Ellen; McKelvie, Jennifer; Pike, Kurt G.; Roberts, Bryan; Rowlinson, Rachel; Smith, James M.; Stockley, Martin; Swarbrick, Martin E.; Treinies, Iris; Waring, Michael J. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Identification and optimization of a novel series of selective PIP5K inhibitors》.Safety of 3,5-Dibromoaniline The author mentioned the following in the article:

Phosphatidyl inositol (4,5)-bisphosphate (PI(4,5)P2) plays several key roles in human biol. and the lipid kinase that produces PI(4,5)P2, PIP5K, has been hypothesized to provide a potential therapeutic target of interest in the treatment of cancers. To better understand and explore the role of PIP5K in human cancers there remains an urgent need for potent and specific PIP5K inhibitor mols. Following a high throughput screen of the AstraZeneca collection, a novel, moderately potent and selective inhibitor of PIP5K, 1, was discovered. Detailed exploration of the SAR for this novel scaffold resulted in the considerable optimization of both potency for PIP5K, and selectivity over the closely related kinase PI3Kα, as well as identifying several opportunities for the continued optimization of drug-like properties. As a result, several high quality in vitro tool compounds were identified (8, 20 and 25) that demonstrate the desired biochem. and cellular profiles required to aid better understanding of this complex area of biol.3,5-Dibromoaniline(cas: 626-40-4Safety of 3,5-Dibromoaniline) was used in this study.

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Safety of 3,5-Dibromoaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《New Synthesis of 2-Oxoalkanamide Oximes》 were Mantrov, S. N.; Lapina, Yu. M.; Shukhtina, E. A.. And the article was published in Russian Journal of Organic Chemistry in 2019. Name: 3,5-Dibromoaniline The author mentioned the following in the article:

Reactions of α-halocarboxylic acid amides R1NHC(O)CH(X)R (R = H, Me, Bu; R1 = C6H5, 4-BrC6H4, 1,3-thiazol-2-yl, etc.; X = Cl, Br) with 3 equiv of hydroxylamine hydrochloride in the presence of bases involves formation of products of nucleophilic substitution of the halogen atom and their subsequent oxidation to the corresponding oximes R1NHC(O)C(=NOH)R. This one-pot transformation can be accomplished in various aprotic solvents or ethanol at 80°C. DMSO as solvent ensures the highest selectivity for the oxidation products. The yields of N-substituted 2-(hydroxyimino)carboxylic acid amides range from 22 to 92%. The results came from multiple reactions, including the reaction of 3,5-Dibromoaniline(cas: 626-40-4Name: 3,5-Dibromoaniline)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Name: 3,5-Dibromoaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases》 were Pemberton, Orville A.; Jaishankar, Priyadarshini; Akhtar, Afroza; Adams, Jessie L.; Shaw, Lindsey N.; Renslo, Adam R.; Chen, Yu. And the article was published in Journal of Medicinal Chemistry in 2019. Application In Synthesis of 3,5-Dibromoaniline The author mentioned the following in the article:

Gram-neg. pathogens expressing serine β-lactamases (SBLs) and metallo-β-lactamases (MBLs), especially those with carbapenemase activity, threaten the clin. utility of almost all β-lactam antibiotics. Here we describe the discovery of a heteroaryl phosphonate scaffold that exhibits noncovalent cross-class inhibition of representative carbapenemases, specifically the SBL KPC-2 and the MBLs NDM-1 and VIM-2. The most potent lead, compound 16, exhibited low nM to low μM inhibition of KPC-2, NDM-1, and VIM-2. Compound 16 potentiated imipenem efficacy against resistant clin. and laboratory bacterial strains expressing carbapenemases while showing some cytotoxicity toward human HEK293T cells only at concentrations above 100μg/mL. Complex structures with KPC-2, NDM-1, and VIM-2 demonstrate how these inhibitors achieve high binding affinity to both enzyme classes. These findings provide a structurally and mechanistically new scaffold for drug discovery targeting multidrug resistant Gram-neg. pathogens and more generally highlight the active site features of carbapenemases that can be leveraged for lead discovery. The experimental part of the paper was very detailed, including the reaction process of 3,5-Dibromoaniline(cas: 626-40-4Application In Synthesis of 3,5-Dibromoaniline)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Application In Synthesis of 3,5-Dibromoaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yu, Yancheng; Yu, Quanwei; Liu, Simeng; Wu, Chenyang; Zhang, Xiaojin published an article in 2021. The article was titled 《Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation》, and you may find the article in European Journal of Medicinal Chemistry.COA of Formula: C6H5Br2N The information in the text is summarized as follows:

Hypoxia-inducible factor-2 (HIF-2), a heterodimeric transcriptional protein consisting of HIF-2α and aryl hydrocarbon receptor nuclear translocator (ARNT) subunits, has a broad transcriptional profile that plays a vital role in human oxygen metabolism M1001, a HIF-2 agonist identified by high-throughput screening (HTS), is capable of altering the conformation of Tyr281 of the HIF-2α PAS-B domain and enhancing the affinity of HIF-2α and ARNT for transcriptional activation. M1002, an analog of M1001, shows improved efficacy than M1001. However, the cocrystal structure of M1001 and HIF-2 has some defects in revealing the agonist binding mode due to the relatively low resolution, while the binding mode of M1002 remained unexplored. To in-depth understand agonist binding profiles, herein, the mol. dynamic (MD) simulations was applied to construct a stable agonist-protein model, and a possible binding mode was proposed through the anal. of the binding free energy and hydrogen bonding of the simulation results. Nine compounds were then synthesized and evaluated to verify the proposed binding mode. Among them, compound 10 manifested improved agonistic activity and reduced toxicity compared to M1002. This study provides deep insight into the binding mode of such HIF-2 agonists, which would be useful for designing novel agonists for HIF-2. The experimental part of the paper was very detailed, including the reaction process of 3,5-Dibromoaniline(cas: 626-40-4COA of Formula: C6H5Br2N)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.COA of Formula: C6H5Br2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Computed Properties of C6H5Br2NIn 2020 ,《Stafia-1: a STAT5a-Selective Inhibitor Developed via Docking-Based Screening of in Silico O-Phosphorylated Fragments》 was published in Chemistry – A European Journal. The article was written by Natarajan, Kalaiselvi; Mueller-Klieser, Daniel; Rubner, Stefan; Berg, Thorsten. The article contains the following contents:

We present a new approach for the identification of inhibitors of phosphorylation-dependent protein-protein interaction domains, in which phenolic fragments are adapted by in silico O-phosphorylation before docking-based screening. From a database of 10 369 180 compounds, we identified 85 021 natural product-derived phenolic fragments, which were virtually O-phosphorylated and screened for in silico binding to the STAT3 SH2 domain. Nine screening hits were then synthesized, eight of which showed a degree of in vitro inhibition of STAT3. After anal. of its selectivity profile, the most potent inhibitor was then developed to Stafia-1, the first small mol. shown to preferentially inhibit the STAT family member STAT5a over the close homolog STAT5b. A phosphonate prodrug based on Stafia-1 inhibited STAT5a with selectivity over STAT5b in human leukemia cells, providing the first demonstration of selective in vitro and intracellular inhibition of STAT5a by a small-mol. inhibitor. The experimental process involved the reaction of 3,5-Dibromoaniline(cas: 626-40-4Computed Properties of C6H5Br2N)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Computed Properties of C6H5Br2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Product Details of 626-40-4In 2016 ,《Substituted quinolines as noncovalent proteasome inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were McDaniel, Tanner J.; Lansdell, Theresa A.; Dissanayake, Amila A.; Azevedo, Lauren M.; Claes, Jacob; Odom, Aaron L.; Tepe, Jetze J.. The article conveys some information:

Screening of a library of diverse heterocyclic scaffolds identified substituted quinolines as inhibitors of the human proteasome. The heterocyclic library was prepared via a novel titanium-catalyzed multicomponent coupling reaction, which rendered a diverse set of isoxazoles, pyrimidines, pyrroles, pyrazoles and quinolines. SAR of the parent lead compound indicated that hydrophobic residues on the benzo-moiety significantly improved potency. Lead compound 3-cyclohexenyl-2-methyl-6-piperidinylquinoline (25) inhibits the chymotryptic-like proteolytic activity of the proteasome (IC50 5.4 μM), representing a new class of nonpeptidic, noncovalent proteasome inhibitors. After reading the article, we found that the author used 3,5-Dibromoaniline(cas: 626-40-4Product Details of 626-40-4)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Product Details of 626-40-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Design, Synthesis and Biological Evaluation of Carbazole Derivatives as Antitubercular and Antibacterial Agents》 were Sellamuthu, Satheeshkumar; Bhat, Mohammad F.; Kumar, Ashok; Nath, Gopal; Singh, Sushil K.. And the article was published in Current Bioactive Compounds in 2019. Electric Literature of C6H5Br2N The author mentioned the following in the article:

Background: The neuroleptic chlorpromazine has been reported for antitubercular activity but the associated antipsychotic activity restricted its clin. presentation. Objectives: Novel derivatives of carbazole having structural similarity with chlorpromazine were designed, in an attempt to reduce the associated side effects, while retaining the antitubercular activity. Materials and Methods: The designed mols. were synthesized and screened for antitubercular and antibacterial activities. The blood-brain barrier (BBB) permeability and mammalian cell (VERO) cytotoxicity (CC50) were examined to determine the safety of compounds Results: Among the developed compounds, 14c, 15c, 16c and 17c were found to be promising against Mtb H37Rv at MIC of 1.56 mug/mL. They were also effective against S. aureus and E. coli at MIC of 0.98 and 7.81 mug/mL, resp. The BBB permeability of the compounds was found to be less than chlorpromazine. Therefore, the developed compounds are expected to have diminished antipsychotic effect. The compounds were further marked safe against mammalian VERO cells at CC50 > 90 mug/mL. Conclusion: The profound antitubercular activity with a concomitant reduction in BBB permeability of carbazole derivatives can pave new vista in the discovery of antitubercular drugs. In addition to this study using 3,5-Dibromoaniline, there are many other studies that have used 3,5-Dibromoaniline(cas: 626-40-4Electric Literature of C6H5Br2N) was used in this study.

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Electric Literature of C6H5Br2N

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary