Category: bromides-buliding-blocks

On December 31, 2020, Holanda, Vanderlan Nogueira; Vicente da Silva, Welson; Henrique do Nascimento, Pedro; Silva, Sergio Ruschi Bergamachi; Cabral Filho, Paulo Euzebio; Assis, Shalom Porto de Oliveira; Augusto da Silva, Cesar; Nascimento de Oliveira, Ronaldo; Queiroz de Figueiredo, Regina Celia Bressan; Lima, Vera Lucia de Menezes published an article.SDS of cas: 574-98-1 The title of the article was Antileishmanial activity of 4-phenyl-1-[2-(phthalimido-2-yl)ethyl]-1H-1,2,3-triazole (PT4) derivative on Leishmania amazonensis and Leishmania braziliensis: In silico ADMET, in vitro activity, docking and molecular dynamic simulations. And the article contained the following:

Organic compounds obtained by click chem. reactions have demonstrated a broad spectrum of biol. activities being widely applied for the development of mols. against pathogens of medical and veterinary importance. Cutaneous leishmaniasis (CL), caused by intracellular protozoa parasite of genus Leishmania, comprises a complex of clin. manifestations that affect the skin and mucous membranes. The available drugs for the treatment are toxic and costly, with long periods of treatment, and the emergence of resistant strains has been reported. In this study we investigated the in vitro effects of a phthalimide-1,2,3-triazole derivative, the 4-Phenyl-1-[2-(phthalimido-2-yl)ethyl]-1H-1,2,3-triazole (PT4) obtained by click chem., on mammalian cells and on L. amazonensis and L. braziliensis, the causative agents of CL in Brazil. In silico ADMET evaluation of PT4 showed that this mol. has good pharmacokinetic properties with no violation of Lipinski’s rules. The in vitro assays showed that PT4 was more selective for both Leishmania species than to mammalian cells. This compound also presented low cytotoxicity to mammalian cells with CC50 > 500μM. Treatment of promastigote forms with different concentrations of PT4 resulted in ultrastructural alterations, such as plasma membrane wrinkling, shortening of cell body, increased cell volume and cell rupture. The mol. dynamic simulations showed that PT4 interacts with Lanosterol 14 α-demethylase from Leishmania, an essential enzyme of lipid synthesis pathway in this parasite. Our results demonstrated PT4 was effective against both species of Leishmania. PT4 caused a decrease of mitochondrial membrane potential and increased production of reactive oxygen species, which may lead to parasite death. Taken together, our results pointed PT4 as promissing therapeutic agent against CL. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to leishmaniasis chemotherapy pthalimide click chem leishmania, 1,2,3-triazole, chemotherapy, click chemistry, leishmaniasis, phthalimide, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kurogi, Takashi; Chu, Jiaxiang; Chen, Yaofeng; Mindiola, Daniel J. published an article in 2019, the title of the article was Neutral and Anionic Monomeric Zirconium Imides Prepared via Selective C=N Bond Cleavage of a Multidentate and Sterically Demanding β-Diketiminato Ligand.HPLC of Formula: 574-98-1 And the article contains the following content:

A sterically encumbering multidentate β-diketiminato ligand, tBuL2 (tBuL2=[ArNC(tBu)CHC(tBu)NCH2CH2N(Me)CH2CH2NMe2]-, Ar = 2,6-iPr2C6H3), is reported in this study along with its coordination chem. to zirconium(IV). Using the lithio salt of this ligand, Li(tBuL2) (4), the zirconium(IV) precursor (tBuL2)ZrCl3 (6) could be readily prepared in 85% yield and structurally characterized. Reduction of 6 with 2 equiv of KC8 gave the terminal and mononuclear zirconium imide-chloride [C(tBu)CHC(tBu)NCH2CH2N(Me)CH2CH2NMe2]Zr(=NAr)(Cl) (7) as the result of reductive C=N cleavage of the imino fragment in the multidentate ligand tBuL2 by an elusive ZrII species (tBuL2)ZrCl (A). The azabutadienyl ligand in 7 can be further reduced by 2 e- with KC8 to afford the anionic imide [K(THF)2]{[CH(tBu)CHC(tBu)NCH2CH2N(Me)CH2CH2N(Me)CH2]Zr = NAr} (8-2THF) in 42% isolated yield. Complex 8-2THF results from the oxidative addition of an amine C-H bond followed by migration to the vinylic group of the formal [C(tBu)CHC(tBu)NCH2CH2N(Me)CH2CH2NMe2]- ligand in 7. All halides in 6 can be replaced with azides to afford (tBuL2)Zr(N3)3 (9) which was structurally characterized, and reduction with two equiv of KC8 also results in C=N bond cleavage of tBuL2 to form [C(tBu)CHC(tBu)NCH2CH2N(Me)CH2CH2NMe2]Zr(=NAr)(N3) (10), instead of the expected azide disproportionation to N3- and N2. Solid-state single crystal structural studies confirm the formation of mononuclear and terminal zirconium imido groups in 7, 8-Et2O, and 10 with Zr = NAr distances being 1.8776(10), 1.9505(15), and 1.881(3) Å, resp. 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 zirconium lithium diketiminato azide complex preparation crystal structure, azides, imides, reduction, zirconium, Inorganic Chemicals and Reactions: Coordination Compounds and other aspects.HPLC of Formula: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 1, 2019, Holub, Jan; Santoro, Antonio; Lehn, Jean-Marie published an article.Product Details of 574-98-1 The title of the article was Electronic absorption and emission properties of bishydrazone [2 × 2] metallosupramolecular grid-type architectures. And the article contained the following:

Several ditopic ligands containing two tridentate bishydrazone coordination subunits and their Zn(II) and Cd(II) [2 × 2] grid-type complexes were prepared and their photoluminescent properties studied. A special attention was devoted to the influence of the orientation of the hydrazone group N-N=in the core of the ligands and their complexes. Its reversal from [pyridine=N-N-pyrimidine] (L1) to [pyridine-N-N=pyrimidine] (L2) has a strong impact on the observed absorption and emission behavior of particular ligands (L1 and L2) as well as of their [2 × 2] grid assemblies. The further lateral functionalization of the ligands led to different emission quantum yields of the resulting grids, while their emission and absorption spectra varied very little. The simplest derivative L1 turned out to have the best performance with, for its Zn(II) complex, relatively high quantum yield 60%. 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 zinc cadmium hydrazone grid complex preparation, crystal structure zinc cadmium hydrazone grid, Inorganic Chemicals and Reactions: Coordination Compounds and other aspects.Product Details of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 7, 2019, Wang, Guoqiang; Shen, Ruichao; Granger, Brett; He, Jing; Xing, Xuechao; He, Yong; Long, Jiang; Ma, Jun; Wang, Bin; Or, Yat Sun published a patent.COA of Formula: C9H9BrO3 The title of the patent was Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof. And the patent contained the following:

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: I which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which is associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-l associated with hepatic steatosis, including non-alc. fatty liver disease (NAFLD) and non-alc. steatohepatitis (NASH). The experimental process involved the reaction of 5-Bromo-2-methoxy-4-methylbenzoic acid(cas: 90326-61-7).COA of Formula: C9H9BrO3

The Article related to tetrazole apoptosis signal regulating kinase 1 inhibitors nafld nash, ask1 mediated liver kidney autoimmune neurodegenerative inflammatory cardiovascular diseases, Pharmacology: Drug Interactions and General Pharmacology and other aspects.COA of Formula: C9H9BrO3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 6, 2019, Yang, Xianteng; Wang, Fan; Zhu, Hua; Yang, Zhi; Chu, Taiwei published an article.SDS of cas: 574-98-1 The title of the article was Synthesis and Bioevaluation of Novel [18F]FDG-Conjugated 2-Nitroimidazole Derivatives for Tumor Hypoxia Imaging. And the article contained the following:

Hypoxia imaging can guide tumor treatment and monitor changes in hypoxia during treatment. However, there is still no ideal hypoxia imaging agent for clin. applications. In this study, two novel 2-nitromidazole derivatives were synthesized and directly radiolabeled by [18F]FDG in high radiochem. yield and excellent radiochem. purity. Cell experiments, biodistribution, and positron emission tomog. (PET) imaging studies were also conducted in mice-bearing S180 or OS732 tumors. [18F]FDG-2NNC2ON [(2R,3S,4R,E)-2-18F-fluoro-3,4,5,6-tetrahydroxyhexanal O-3-(2-(2-nitro-1H-imidazole-1-yl)ethylamino)-2-oxopropyl oxime] and [18F]FDG-2NNC5ON [(2R,3S,4R,E)-2-18F-fluoro-3,4,5,6-tetrahydroxyhexanal-O-3-(5-(2-nitro-1H-imidazole-1-yl)pentylamino)-2-oxopropyl oxime] can be cleared from the blood quickly and specifically target hypoxic tumor cells. The uptake of the probes by hypoxic cells gradually increases with time. After 4 h, the uptake value of [18F]FDG-2NNC2ON in hypoxic cells is 3.2 times higher than that in normoxia cells. In contrast, there is no difference in the uptake of [18F]FDG between hypoxic cells and normoxia cells. Biodistribution resulting from two tumor models indicate that the uptake values of the two radiotracers in the tumor are higher at 1 h than those at 2 and 4 h. At 1 and 2 h, the tumors are clearly observed on the PET images and the imaging features of [18F]FDG-2NNC5ON and [18F]FDG-2NNC2ON are distinct from those of [18F]FDG. Compared with [18F]FDG-2NNC5ON, [18F]FDG-2NNC2ON has a higher proportion of renal excretion, lower digestive tract uptake, and better imaging contrast because of its higher hydrophilicity. At 2 h, [18F]FDG-2NNC2ON shows a good tumor-to-blood (T/B) ratio, tumor-to-muscle ratio based on biodistribution (Bio-T/M ratio), and tumor-to-muscle ratio based on regions of interest on the PET images [region of interest (ROI)-T/M ratio] in the two tumor models (T/B, Bio-T/M, and ROI-T/M ratios are 3.2, 2.6, and 3.9 in the S180 tumor model and are 3.4, 4.2, and 4.6 in the OS732 tumor model, resp.). The imaging features visualized with autoradiog. mostly coincided with the pos. areas of HIF1α staining by immunofluorescence. Meanwhile, the biodistribution study and PET imaging revealed that the uptake of the radiotracers in the tumor cannot be competed by 5% glucose, confirming that [18F]FDG-2NNC2ON targets the hypoxic regions of the tumors instead of targeting tumors through the glucose metabolism pathway. These results suggest that the new 2-nitroimidazole derivative conjugated with [18F]FDG, [18F]FDG-2NNC2ON, has potential as an imaging agent for hypoxia. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to radiofluorine fdg nitroimidazole derivative preparation tumor hypoxia pet imaging, 2-nitroimidazole, [18f]fdg, hypoxia imaging, tumor, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2018, Lin, Xiao; Ruan, Qing; Lin, Ling; Zhang, Xuran; Duan, Xiaojiang; Teng, Yanguo; Zhang, Junbo published an article.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Biological evaluation and SPECT imaging of tumor hypoxia using a novel technetium-99m labeled tracer with 2-nitroimidazole moiety. And the article contained the following:

To develop novel 99mTc labeled nitroimidazole imaging agents for imaging tumor hypoxia, 99mTc labeled ethylene diamine tetraacetic acid derivative of 4-nitroimidazole was reported by us earlier, which showed disadvantage of an unsatisfactory tumor-to-blood ratio. Therefore, 2-nitroimidazole was adopted as a pharmacophore to synthesize EDTA-2-EtNHNM, which was radiolabeled with 99mTc in high yield to achieve 99mTc-EDTA-2-EtNHNM. 99mTc-EDTA-2-EtNHNM was hydrophilic and exhibited good in vitro stability. Cellular experiment demonstrated its hypoxic selectivity while biodistribution results showed improved tumor-to-blood and tumor-to-muscle ratios. SPECT imaging studies of 99mTc-EDTA-2-EtNHNM indicated obvious accumulation in tumor, suggesting its potential to be a radiotracer for imaging tumor hypoxia. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to spect imaging tumor hypoxia technetium 99m nitroimidazole, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 30, 2019, Bathula, Chinna; Mallikarjuna, K.; Kadam, Abhijit; Shrestha, Nabeen K.; Khadtare, Shubhangi; Mane, Suresh D.; Kim, Haekyoung published an article.HPLC of Formula: 41819-13-0 The title of the article was Synthesis and photophysical investigations of pyromellitic diimide based small molecules. And the article contained the following:

The present work reports on the highly efficient microwave assisted Suzuki coupling reaction for obtaining pyromellitic diimide based sym. small mols. with donor-acceptor-donor (D-A-D) configuration. Electron rich bithiophene is employed as a donor and alkyl substituted pyromellitic diimide units are explored as acceptors to get the desired small mols. In order to study the relation between chem. structures and material properties, the prepared compounds were characterized in detail using absorption spectroscopy, cyclic voltammetry and thermograviometric anal. The compounds exhibited good thermal stabilities with high decomposition temperature Photophys. investigations of the newly synthesized pyromellitic diimide based small mols., suggests these materials as potential candidates for organic electronic applications. The experimental process involved the reaction of 3,6-Dibromobenzene-1,2,4,5-tetracarboxylic acid(cas: 41819-13-0).HPLC of Formula: 41819-13-0

The Article related to pyromellitic diimide bithiophene compound preparation thermal stability electrochem luminescence, Heterocyclic Compounds (One Hetero Atom): Thiophenes and other aspects.HPLC of Formula: 41819-13-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 1, 2008, Ju-Nam, Yon; Allen, David W.; Gardiner, Philip H. E.; Bricklebank, Neil published an article.Electric Literature of 83152-22-1 The title of the article was ω-Thioacetylalkylphosphonium salts: Precursors for the preparation of phosphonium-functionalised gold nanoparticles. And the article contained the following:

Two new ω-thioacetylalkylphosphonium salts that function as masked cationic alkanethiolate ligands for the stabilization of gold nanoparticles were prepared Both (3-thioacetylpropyl)triphenylphosphonium bromide and (6-thioacetylhexyl)triphenylphosphonium bromide form water-soluble gold nanoparticles of ∼5-10 nm in size that are stable for up to six months. The related (3-thioacetylpropyl)diphenylphosphine oxide was also prepared but did not act as a stabilizing ligand in gold nanoparticle formation. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Electric Literature of 83152-22-1

The Article related to phosphonium functionalized gold nanoparticle, Surface Chemistry and Colloids: Solid-Liquid Systems and other aspects.Electric Literature of 83152-22-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 17, 2014, Li, Yun-Long; Burns, David M.; Feng, Hao; Xue, Chu-Biao; Wang, Anlai; Pan, Jun published a patent.HPLC of Formula: 1196157-51-3 The title of the patent was Preparation of bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors for treating proliferative and immune disorders. And the patent contained the following:

The present disclosure describes bicyclic aromatic carboxamide derivatives of formula I (wherein Cy is (un)substituted C3-7 cycloalkyl or (un)substituted 4-10 membered heterocycloalkyl; A1 is N or (un)substituted CH; R2 is H, halogen, C1-6 alkyl, etc.; or A1 and R2 together form part of a ring; R3 is H, halogen or NH2; R4 is H or halogen; and A5-A8 are independently N or (un)substituted CH, with provisos), as well as their compositions and methods of use as Pim kinase inhibitors for treating cancer and other diseases. Synthetic procedures for preparing I are exemplified. Example compound II was prepared in a 6-step synthesis that involved reaction of intermediate III with benzyl [(3S)-1-(3-aminopyridin-4-yl)piperidin-3-yl]carbamate followed by deprotection of the intermediate formed to give II. In Pim kinase inhibitory assays in vitro, II had IC50 values of ≤100 nM for Pim1 and Pim3 and an IC50 value between 100 nM and 1000 nM for Pim2 kinase. The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).HPLC of Formula: 1196157-51-3

The Article related to preparation bicyclic aromatic carboxamide compound pim kinase inhibitor therapy, proliferative immune disorder treatment bicyclic aromatic carboxamide compound, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 1196157-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 29, 2001, Astles, Peter C.; Eastwood, Paul R.; Houille, Olivier; Levell, Julian; Pauls, Heinz; Czekaj, Mark; Liang, Guyan; Gong, Yong; Pribish, James; Neuenschwander, Kent published a patent.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene The title of the patent was Preparation of (hetero)arylacyl-piperidinyl-benzylamines for use as tryptase inhibitors. And the patent contained the following:

Title compounds I [Ar = (hetero)aryl, where the two groups on the Ar ring are β to each other; R1-2 = H, alkyl; R3 = (un)substituted(hetero)aryl, arylalkenyl, cycloalkenyl, cycloalkyl, etc.; R4 = H, acyl, alkoxy, alkyloxycarbonyl, carboxy, CN, halo, etc.; n = 0 – 4] were prepared Over 300 synthetic examples were disclosed. For instance, 3-bromobenzylbromide was converted in two steps to boronate II. II was coupled to the triflate ester derivative of the enol of 4-oxo-N-benzyloxycarbonylpiperidine (DMF, K2CO3, PdCl2(dppf)•CH2Cl2, 80°C, 18 h) to give the corresponding bicyclic intermediate. This intermediate was deprotected and reduced to the piperidine (EtOH, 10% Pd-C/H2, room temperature, 5 h) and coupled to 5-phenethylthiophene-2-carboxylic acid (DMF, HAPyU, iPr2NEt, room temperature, 18 h) to give III. III had Ki = 50 nM for tryptase. I are useful in the treatment of e.g., asthma and inflammatory diseases. The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene

The Article related to piperidinylbenzylamine tryptase inhibitor preparation, pyridine quinoline thiophene furan indole piperidine tryptase inhibitor preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary