Category: 574-98-1

Varano, Flavia; Catarzi, Daniela; Vigiani, Erica; Vincenzi, Fabrizio; Pasquini, Silvia; Varani, Katia; Colotta, Vittoria published an article in 2020, the title of the article was Piperazine- and piperidine-containing thiazolo[5,4-d]pyrimidine derivatives as new potent and selective adenosine A2A receptor inverse agonists.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

The therapeutic use of A2A adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A2A AR antagonists to avoid both immunoescaping of tumor cells and tumor development is well documented. Herein, authors report on the synthesis and biol. evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Binding and potency data indicated that a good number of potent and selective hA2A AR inverse agonists were found. Amongst them, the compound I exhibited the highest A2A AR binding affinity (Ki = 8.62 nM) as well as inverse agonist potency (IC50 = 7.42 nM). The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to piperazinyl piperidinyl thiazolopyrimidine preparation in silico adme prediction, adenosine a2a receptor inverse agonist human, g protein-coupled receptors, adenosine a2a receptor ligands, adenosine receptors, thiazolo[5,4-d]pyrimidines and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2022, Ekinci, Orhan; Akkoc, Mitat; Khan, Siraj; Yasar, Sedat; Guerses, Canbolat; Noma, Samir; Balcioglu, Sevgi; Sen, Betuel; Ayguen, Muhittin; Yilmaz, Ismet published an article.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Synthesis and biological evaluation of Au-NHC complexes. And the article contained the following:

New seven Au-N-heterocyclic carbene (NHC) complexes were synthesized via transmetalation from Ag-NHC complexes. NHC salts, Ag-NHC, and Au-NHC complexes were fully characterized by widely used spectroscopic techniques. The mol. and crystal structures of 3b and 3f Au-NHC complexes were clarified through the single-crystal x-ray diffraction method. According to x-ray diffraction anal. results, the coordination geometry around Au(I) atoms in the complexes are revealed to be almost linear with C-Au-Cl angle. Anticancer activity, DNA binding, xanthine oxidase (XO) inhibitory activity studies, and mol. docking studies were evaluated for all Au-NHC complexes to explore the binding mechanism at the active site. The IC50 value of Au-NHC complexes against human colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines was defined by MTT assay. The IC50 values for MCF-7 in the range of 5.2 ± 2 to 152.4 ± 1μM and Caco-2 5.2 ± 1 to 152.7 ± 2μM showed that 3a, 3b, 3c, 3d, and 3g have better anticancer activity than Cisplatin incredibly complex 3a against both cancer cell line. All Au-NHC complexes showed excellent antimicrobial activity against different bacteria and fungi. 3a was the complex that exhibited the best antimicrobial activity here as well. The XO inhibitory activity exptl. results indicated that all gold complexes showed remarkable inhibition activity against XO compared to the generally used standard, allopurinol. The range of IC50 value was determined from 0.407 to 2.681μM. 3d complex showed the lowest IC50 value at 0.407μM. DNA binding experiments were performed using agarose gel electrophoresis to observe the ability of synthesized Au-NHC complexes to interact with the supercoiled pUC19 plasmid DNA. Mol. docking studies were performed to determine the binding mode of all active compounds against the XO enzyme, antibacterial, antifungal, and MCF-7 cell lines. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to silver gold heterocyclic carbene complex halo preparation crystal structure, antitumor human silver gold heterocyclic carbene complex halo, antibacterial antifungal silver gold heterocyclic carbene complex halo dna and other aspects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 17, 2020, Gonzalez-Rodriguez, Jorge; Soto, Martin; Soengas, Raquel G.; Rodriguez-Solla, Humberto published an article.Category: bromides-buliding-blocks The title of the article was SmI2-promoted cross coupling reaction of N-2-bromoethylphthalimide and carbonyl compounds: Synthesis of α-aryl-α’-hydroxy ketones. And the article contained the following:

In this paper, the SmI2-mediated carbonyl-imide reductive cross coupling between N-2-bromoethylphthalimide and different aldehydes and ketones in the presence of anhydrous catalytic NiI2 was disclosed. This methodol. provided an effective tool to prepare α-aryl-α’-hydroxy ketones I [R1 = n-C7H15, 4-ClC6H4, C6H4CH=CH, etc; R1 = R2 = Et; R1R2 = (CH2)4, (CH2)5] under mild conditions which could be applied to various functionalized, aliphatic and aromatic aldehydes and ketones. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to aryl alpha hydroxy ketone preparation chemoselective, bromoethylphthalimide aldehyde reductive cross coupling samarium iodide mediated, ketone bromoethylphthalimide reductive cross coupling samarium iodide mediated and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 31, 2020, Dato, Florian M.; Neudoerfl, Joerg-Martin; Guetschow, Michael; Goldfuss, Bernd; Pietsch, Markus published an article.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was ω-Quinazolinonylalkyl aryl ureas as reversible inhibitors of monoacylglycerol lipase. And the article contained the following:

The serine hydrolase monoacylglycerol lipase (MAGL) is involved in a plethora of pathol. conditions, in particular pain and inflammation, various types of cancer, metabolic, neurol. and cardiovascular disorders, and is therefore a promising target for drug development. Although a large number of irreversible-acting MAGL inhibitors have been discovered over the past years, there are only few compounds known so far which inhibit the enzyme in a reversible manner. Therefore, much effort is put into the development of novel chem. entities showing reversible inhibitory behavior, which is thought to cause less undesired side effects. To explore a wide range of chem. structures as MAGL binders, we have applied a virtual screening approach by docking small mols. into the crystal structure of human MAGL (hMAGL) and envisaged a library of 45 selected compounds which were then synthesized. Biochem. investigations included the determination of the inhibitory potency on hMAGL and two related hydrolases, i.e. human fatty acid amide hydrolase (hFAAH) and murine cholesterol esterase (mCEase). The most promising candidates from theses analyses, i.e. three ω-quinazolinonylalkyl aryl ureas bearing alkyl spacers of three to five methylene groups, exhibited IC50 values of 20-41μM and reversible, detergent-insensitive behavior towards hMAGL. Among these compounds, the inhibitor 1-(3,5-bis(trifluoromethyl)phenyl)-3-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)butyl)urea (96) was selected for further kinetic characterization, yielding a dissociation constant Ki = 15.4μM and a mixed-type inhibition with a pronounced competitive component (α = 8.94). This mode of inhibition was further supported by a docking experiment, which suggested that the inhibitor occupies the substrate binding pocket of hMAGL. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to quinazolinonylalkyl aryl urea inhibitor monoacylglycerol lipase, cholesterol esterase, enzyme kinetics, fatty acid amide hydrolase, inhibitors, monoacylglycerol lipase, promiscuous inhibition, serine hydrolases and other aspects.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

McGrory, Rochelle; Faggyas, Reka J.; Sutherland, Andrew published an article in 2021, the title of the article was One-pot synthesis of N-substituted benzannulated triazoles via stable arene diazonium salts.HPLC of Formula: 574-98-1 And the article contains the following content:

A mild and effective one-pot synthesis of benzothiatriazine-1,1(2H)-dioxides I [R = Me, Bn, Ph, etc.] and 1,2,3-benzotriazin-4(3H)-ones II [R1 = H, 5-F, 7-CF3, etc.; R2 = H, cyclohexyl, Ph, etc.] was developed. The method involved the diazotization and subsequent cyclization of 2-aminobenzamides and 2-aminobenzenesulfonamides via stable diazonium salts, prepared using a polymer-supported nitrite reagent and p-tosic acid. The transformation was compatible with a wide range of aryl functional groups and amide/sulfonamide-substituents and was used for the synthesis of pharmaceutically important targets. The synthetic utility of the one-pot diazotizaton-cyclization process was further demonstrated with the preparation of an α-amino acid containing 1,2,3-benzotriazin-4(3H)-one. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).HPLC of Formula: 574-98-1

The Article related to benzotriazinone preparation, aminobenzamide polymer supported nitrite diazotizaton cyclization, benzothiatriazine dioxide preparation, aminobenzenesulfonamide polymer supported nitrite diazotizaton cyclization and other aspects.HPLC of Formula: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Asadi, Mehdi; Ebrahimi, Mostafa; Mohammadi-Khanaposhtani, Maryam; Azizian, Homa; Sepehri, Saghi; Nadri, Hamid; Biglar, Mahmood; Amanlou, Massoud; Larijani, Bagher; Mirzazadeh, Roghieh; Edraki, Najmeh; Mahdavi, Mohammad published an article in 2019, the title of the article was Design, synthesis, molecular docking, and cholinesterase inhibitory potential of phthalimide-dithiocarbamate hybrids as new agents for treatment of Alzheimer’s disease.Product Details of 574-98-1 And the article contains the following content:

A novel series of phthalimide-dithiocarbamate hybrids was synthesized and evaluated for in vitro inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The anti-cholinesterase results indicated that among the synthesized compounds, the compounds 7g and 7h showed the most potent anti-AChE and anti-BuChE activities, resp. Mol. docking and dynamic studies of the compounds 7g and 7h, resp., in the active site of AChE and BuChE revealed that these compounds as well interacted with studied cholinesterases. These compounds also possessed drug-like properties and were able to cross the BBB. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Product Details of 574-98-1

The Article related to synthesis docking cholinesterase inhibitor phthalimide dithiocarbamate hybrid antialzheimer, alzheimer’s disease, acetylcholinesterase, butyrylcholinesterase, dithiocarbamate, inhibitory activity, phthalimide and other aspects.Product Details of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 5, 2020, Sidhu, Jagpreet Singh; Raj, Pushap; Pandiyan, Thangarasu; Singh, Narinder published an article.Formula: C10H8BrNO2 The title of the article was Synthesis of Nickel(II) Complexes of Novel Naphthalimide Based Heterodipodal Schiff Base Ligands, Structure, Characterization and Application for Degradation of Pesticides. And the article contained the following:

To degrade the highly toxic pesticide into less harmful components, authors have synthesized four nickel complexes of naphthalimide based organic ligands. These complexes catalyze the hydrolysis of phosphorothioate bonds of organophosphates in an aqueous medium. The metal complexes {[Ni(L1)2]-[Ni(L4)2]} were synthesized by the electrochem. method and characterized using single-crystal x-ray crystallog. and mass spectrometry. Anal. techniques revealed that complexes are mononuclear and possess octahedral geometry. The rate of degradation of chlorpyriphos and parathion Me was evaluated using 31P NMR and LC-MS chromatogram. The byproduct of chlorpyriphos upon catalytic degradation with complex was confirmed from mass spectrometry. It was found that chlorpyriphos degrade into 3,5,6-trichloropyridin-2-ol after 50 min of incubation with catalyst. However, parathion Me took only 20 min to hydrolyze into its byproduct. Moreover, the inhibition assay of acetylcholinesterase was performed for pesticides in the presence of metal complex and the interesting outcome was recorded. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Formula: C10H8BrNO2

The Article related to nickel naphthalimide heterodipodal schiff base preparation degrade pesticide, crystal mol structure naphthalimide heterodipodal schiff base, phosphorothioate organophosphate hydrolysis catalyst naphthalimide heterodipodal schiff base nickel and other aspects.Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 15, 2021, Rezaei, Mohammad Taher; Keypour, Hassan; Bayat, Mehdi; Soltani, Elham; Jamshidi, Mahdi; Gable, Robert William published an article.Category: bromides-buliding-blocks The title of the article was Synthesis of a tertiary amine by direct reductive amination of a carbonyl compound to form a scorpionate ligand; formation of Mn (II), Zn (II) and Cd (II) complexes, DFT calculations and, molecular docking studies. And the article contained the following:

A hexadentate, asym. tripodal scorpionate type ligand, [[N1-Pyridin-2-ylmethyl-N1-[2-(4-pyridine-2-ylmethyl-piperazine-1-yl)-ethyl]-ethane-1,2-diamine]] (L) was prepared To form this ligand, the direct reductive amination of a carbonyl compound by NaBH4 was used for the synthesis of tertiary amine. The complexes [MnL](ClO4)2, [CdL](ClO4)2, [ZnL](ClO4)2 also were prepared The synthesized compounds were characterized by elemental analyses, FTIR, ESI-MS and, NMR spectroscopy. An X-ray crystal structure of [MnL] (ClO4)2, shows that the coordination environment around the manganese is a distorted trigonal prism. The nature of metal-ligand bonding in the complexes was studied by Natural Bond Orbital anal., Energy Decomposition Anal. and Energy Decomposition Anal. using Natural Orbitals for Chem. Valence variation. Mol. docking was used for the biol. evaluation of the anticancer and antioxidant activities of the synthesized compounds The docking results indicated that the Cd, Mn, and Zn-complexes had the highest binding affinity (MolDock Score) for the binding sites of cytochrome P 450, myeloperoxidase, and cytochrome P 450, resp. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to preparation manganese cadmium zinc scorpionate complex, crystal mol structure manganese cadmium zinc scorpionate complex, mol docking manganese cadmium zinc scorpionate complex, anticancer antioxidant activity manganese cadmium zinc scorpionate complex and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 28, 2019, de O. Assis, Shalom P.; da Silva, Moara T.; da Silva, Filipe Torres; Sant’Anna, Mirella P.; de Albuquerque Tenorio, Carolina M. B.; dos Santos, Caroline F. Brito; da Fonseca, Caique S. M.; Seabra, Gustavo; Lima, Vera L. M.; de Oliveira, Ronaldo N. published an article.Category: bromides-buliding-blocks The title of the article was Design and synthesis of triazole-phthalimide hybrids with anti-inflammatory activity. And the article contained the following:

Phthalimido-alkyl-1H-1,2,3-triazole derivatives were efficiently synthesized using 1,3-dipolar cycloaddition reaction. Anti-inflammatory activity and toxicity studies were performed. The results demonstrated that all the tested compounds reduced carrageenan-induced paw edema and indicated no lethality for toxicity against Artemia salina and acute toxicity in vivo (LD50 up to 1 g kg-1). Furthermore, the structure of phthalimide linked to Ph group proved to be more active than the compounds containing benzothiazole moiety. Structural modifications such as removal of the phthalimide group and subsequent acetylation, to exemplify a non-cyclic amide, demonstrate that the phthalimide and triazole moieties were important for design of potent candidates with anti-inflammatory drug proprieties. Docking into the cyclooxygenase-2 (COX-2) confirmed the importance of the phthalimide and triazole groups in the anti-inflammatory activity. The histopathol. studies showed that the compounds did not cause serious pathol. lesions liver or kidneys. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to benzothiazolyl sulfanyl methyl phthalimidoylalkyl triazole regioselective preparation, phenyl phthalimido alkyl triazole regioselective preparation, antiinflammatory activity sar acute toxicity lipophilicity mol docking, anti-inflammatory activity, phthalimide, toxicity, triazole and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2021, Al-Hamashi, Ayad A.; Chen, Dongxing; Deng, Youchao; Dong, Guangping; Huang, Rong published an article.Application of 574-98-1 The title of the article was Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5. And the article contained the following:

Protein arginine methyltransferases (PRMTs) have been implicated in the progression of many diseases. Understanding substrate recognition and specificity of individual PRMT would facilitate the discovery of selective inhibitors towards future drug discovery. Herein, we reported the design and synthesis of bisubstrate analogs for PRMTs that incorporate a S-adenosylmethionine (SAM) analog moiety and a tripeptide through an alkyl substituted guanidino group. Compound AH237 is a potent and selective inhibitor for PRMT4 and PRMT5 with a half-maximal inhibition concentration (IC50) of 2.8 and 0.42 nmol/L, resp. Computational studies provided a plausible explanation for the high potency and selectivity of AH237 for PRMT4/5 over other 40 methyltransferases. This proof-of-principle study outlines an applicable strategy to develop potent and selective bisubstrate inhibitors for PRMTs, providing valuable probes for future structural studies. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application of 574-98-1

The Article related to amino acids role: bsu (biological study, unclassified), biol (biological study), computational biology, drug design, homo sapiens, human, methylation, molecular docking, molecular modeling, tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgk), tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgr) and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary