Tag: 200-300

On March 31, 2020, Babin, Victor; Tournier, Benjamin B.; Davis, Audrey; Dubost, Emmanuelle; Pigree, Gilbert; Lohier, Jean-Francois; Reboul, Vincent; Cailly, Thomas; Bouillon, Jean-Philippe; Millet, Philippe; Fabis, Frederic published an article.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Design of iodinated radioligands for SPECT imaging of central human 5-HT4R using a ligand lipophilicity efficiency approach. And the article contained the following:

A series of iodinated ligands for the SPECT imaging of 5-HT4 receptors was designed starting from the previously reported hit MR-26132. We focused on the modulation of the piperidine-containing lateral chain by introducing hydrophilic groups in order to decrease the lipophilicity of the new ligands. All the synthesized compounds were tested for their binding affinities on 5-HT4Rs and based on the Ligand Lipophilicity Efficiency approach, compound 13 was further selected for radioiodination with iodine-125 and imaging experiments Compound 13 showed its ability to displace the specific signal of the reference compound [125I]SB-207710 but no significant detection of [125I]13 was observed in vivo in SPECT experiments The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to iodinated radioligand preparation spect imaging 5ht4 receptor lipophilicity, 5-ht(4), lle, radio-iodination, spect imaging, serotonin, Placeholder for records without volume info and other aspects.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ruan, Qing; Gan, Qianqian; Zhang, Xuran; Fang, Sian; Zhang, Junbo published an article in 2021, the title of the article was Preparation and bioevaluation of novel 99mTc-labeled complexes with a 2-nitroimidazole HYNIC derivative for imaging tumor hypoxia.Recommanded Product: 574-98-1 And the article contains the following content:

To develop novel 99mTc-labeled single-photon emission computed tomog. (SPECT) radiotracers for imaging hypoxia, a novel HYNICNM ligand (6-hydrazinonicotinamide (HYNIC) 2- nitroimidazole derivative)was designed and synthesized. Itwas radiolabeledwith technetium-99musing tricine/trisodiumtriphenylphosphine-3,3′′,3′′-trisulfonate (TPPTS), tricine/sodiumtriphenylphosphine-3-monosulfonate (TPPMS) and tricine as co-ligands to obtain [99mTc]Tc-tricine-TPPTS-HYNICNM, [99mTc]Tc-tricine-TPPMS-HYNICNM, and [99mTc]Tc-(tricine)2-HYNICNM, resp. The three technetium-99m complexes were radiolabeled in one step with a high yield (95%) and had good stability in saline and mouse serum. In vitro cellular uptake results showed that these complexes exhibited good hypoxic selectivity. The partition coefficient indicated that they were good hydrophilic complexes, and [99mTc]Tc-tricine-TPPTS-HYNICNM displayed the highest hydrophilicity (-3.02 ± 0.08). The biodistribution in mice bearing S180 tumors showed that [99mTc]Tc-tricine-TPPTS-HYNICNM exhibited higher tumor uptake (1.05 ± 0.27% IA/g); more rapid clearance from the liver, blood, muscle, and other non-target organs; and a higher tumor/non-target ratio, especially for the tumor/liver ratio (1.95), than [99mTc]Tc-tricine-TPPMS-HYNICNM and [99mTc]Tc-(tricine)2-HYNICNM. The results of single-photon emission computed tomog. (SPECT) imaging studies of [99mTc]Tctricine-TPPTS-HYNICNM were in accordance with the biodistribution results, which suggested that [99mTc]Tc-tricine-TPPTS-HYNICNM is a promising agent for imaging tumor hypoxia. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to nitroimidazole technetium hydrazinonicotinamide tumor hypoxia imaging, 2-nitroimidazole, hynic, hypoxia, technetium-99m, tumor, Placeholder for records without volume info and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 15, 2021, Ma, Xiaojun; Sun, Nannan; Li, Xinwei; Fu, Wei published an article.Recommanded Product: 2567-29-5 The title of the article was Discovery of novel N-sulfonamide-tetrahydroisoquinolines as potent retinoic acid receptor-related orphan receptor γt agonists. And the article contained the following:

Cancer immunotherapy has become a research hotspot in recent years. A variety of targets were developed for small mol. immuno-oncol. agents, including retinoic acid-related orphan receptor gamma t (RORγt), chemokine receptor, stimulator of interferon genes (Sting), indoleamine 2,3-dioxygenase (IDO), toll-like receptors (TLR), etc. Among them, the retinoic acid receptor-related orphan receptor γt (RORγt) has gradually attracted more attention in these years. In particular, LYC-55716 (cintirorgon), a small mol. RORγt agonist developed by Lycera, has entered the phase II clin. study. In this work, starting from compound 7, compound 28 was obtained after 4 rounds of compound design, synthesis and SAR studies, which had an EC50 of 0.021 ± 0.002 μM in dual Fluorescence Resonance Energy Transfer (dual-FRET) assay and an EC50 of 0.021 ± 0.002 μM in mouse Th17 cell differentiation assay. It indicated that compound 28 had excellent RORγt agonistic activity and was expected to be developed as a new type of small mol. drug for cancer immunotherapy. The mol. dynamic simulation revealed that the agonist 28 formed a strong HYF triplet intramol. interaction to stabilize H12, which helped RORγt to form the protein-binding site and therefore made the receptor ready to recruit coactivator. When the inverse agonist s27 bound with RORγt, the steric hindrance between s27 and H479 caused the destruction of the HYF triplet, leading to the collapse of H12, thus the transcription function of RORγt was interrupted due to the failure of recruiting a coactivator mol. The triplet HYF in RORγt and the rigidity of 28 and s27 were identified to be the structural determinants for the functional switch of RORγt. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Recommanded Product: 2567-29-5

The Article related to sulfonamide tetrahydroisoquinoline potent retinoic acid receptor, agonists, cancer immunotherapy, inverse agonists, rorγt, Placeholder for records without volume info and other aspects.Recommanded Product: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 12, 2020, Ongwae, George M.; Morrison, Kelly R.; Allen, Ryan A.; Kim, Seonghoon; Im, Wonpil; Wuest, William M.; Pires, Marcos M. published an article.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Broadening Activity of Polymyxin by Quaternary Ammonium Grafting. And the article contained the following:

Bacterial pathogens continue to impose a tremendous health burden across the globe. Here, we describe a novel series of polymyxin-based agents grafted with membrane-active quaternary ammonium warheads to combine two important classes of Gram-neg. antimicrobial scaffolds. The goal was to deliver a targeted quaternary ammonium warhead onto the surface of bacterial pathogens using the outer membrane homing properties of polymyxin. The most potent agents resulted in new scaffolds that retained the ability to target Gram-neg. bacteria and had limited toxicity toward mammalian cells. We showed, using a mol. dynamics approach, that the new agents retained their ability to engage in specific interactions with lipopolysaccharide mols. Significantly, the combination of quaternary ammonium and polymyxin widens the activity to the pathogen Staphylococcus aureus. Our results serve as an example of how two membrane-active agents can be combined to produce a class of novel scaffolds with potent biol. activity. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to polymyxin quaternary ammonium grafting antibiotic, antibiotic, colistin, membrane, polymyxin, quarternary ammonium, Placeholder for records without volume info and other aspects.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 29, 2015, Takahashi, Taichi; Umino, Akinori; Iijima, Daisuke; Takamatsu, Hisayuki published a patent.Product Details of 1160653-94-0 The title of the patent was Novel 2-aminopyridine and 2-aminopyrimidine derivatives and medicinal use thereof. And the patent contained the following:

Provided are compounds that exhibit an excellent autotaxin (ATX) inhibitory effect, etc. and are efficacious as a prophylactic or therapeutic agent for diseases in which ATX participates. Compounds represented by general formula I [ring A = cycloalkyl, heterocyclyl, etc.; Z1-Z4 = C, N; R1 = halo, (halo)alkyl, (halo)alkoxy, aryl, etc.; R2, R3 = H, halo, (halo)alkyl, (halo)alkoxy, aryl; R4 = H, alkyl, halo; R5, R6 = H, OH, halo, etc., (linked via O, CO, etc.); L1 = bond, linear alkylene, cycloalkylene, etc] have an excellent ATX inhibitory effect and are useful as a prophylactic or therapeutic agent for ATX-associated diseases, e.g., tumor, obesity, and inflammation. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methoxybenzaldehyde(cas: 1160653-94-0).Product Details of 1160653-94-0

The Article related to aminopyridine aminopyrimidine preparation autotaxin inhibitor antitumor antiobesity antiinflammation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Product Details of 1160653-94-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 21, 2022, Chehardoli, Gholamabbas; Gholamhoseini, Pooriya; Ebadi, Ahmad; Ziaei, Maral; Akbarzadeh, Tahmineh; Saeedi, Mina; Mahdavi, Mohammad; Khoshneviszadeh, Mehdi; Najafi, Zahra published an article.COA of Formula: C10H8BrNO2 The title of the article was 6-Methoxy-1-tetralone Derivatives Bearing an N-Arylpyridinium Moiety as Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Molecular Docking Study. And the article contained the following:

A novel series of 6-methoxy-1-tetralone derivatives bearing N-aryl pyridinium moiety I (Ar = C6H5, 2-FC6H4, 3-ClC6H4, etc.; n = 1, 2, 3, 4, 5; X = Cl, Br) were designed, synthesized, and evaluated as acetyl and butyrylcholinesterase inhibitors. The designed derivatives inhibited acetylcholinesterase (AChE) with IC50 values of 0.025-23.743μM and butyrylcholinesterase (BChE) with IC50 values of 0.716-20.588μM. The synthesized compounds were divided into two series. Derivatives containing N-benzyl moieties generally were more potent anti-AChE and anti-BChE agents than compounds with N-alkylphthalimide groups. Among them, the compound I (Ar = C6H5; n = 1; X = Br) and compound I (Ar = 3-ClC6H4; n = 1; X = Br) exhibited significant inhibitory activity against AChE and BChE with IC50 values of 0.025 and 0.716μM in comparison to donepezil as a reference drug (0.029 and 0.948μM, resp.). The results of kinetic and mol. modeling studies demonstrated that the synthesized compounds I (Ar = C6H5; n = 1; X = Br) and I (Ar = 3-ClC6H4; n = 1; X = Br) derivatives can act as mixed and dual binding inhibitors, and bind to both CAS and PAS of AChE and BChE enzymes. Among the assessed compounds, the compound I (Ar = C6H5; n = 1; X = Br) indicated significant neuroprotection against H2O2-induced cell death in PC12 cells. So, these findings indicate the therapeutic potential of 6-methoxy-1-tetralone derivatives bearing N-aryl pyridinium moiety derivatives as anti-AD agents. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).COA of Formula: C10H8BrNO2

The Article related to methoxy tetralone aryl pyridinium preparation, mol docking adme inhibitor physicochem property, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 15, 2022, Wang, Tingting; Dong, Jianhao; Yu, Na; Tang, Weiqin; Jin, Yaping; Xu, Yixin; Yang, Jingshuai published an article.Safety of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Synthesis and properties of a new ether-free poly(bis-alkylpiperidinium) polymer for the anion exchange membrane. And the article contained the following:

Developing anion exchange membranes (AEMs) with high performance and excellent alk. stability is a huge challenge to the fuel cell. Herein, a new bispiperidinium compound is synthesized through a nucleophilic reaction between 4,4′-trimethylenebis (1-Me piperidine) and 4-bromomethylbiphenyl. Subsequently, a novel poly(bis-alkylpiperidinium) polymer (i.e. Tmmp-Bmb-TFAc) is synthesized through the Friedel-Crafts polycondensation of bispiperidinium monomer and 1,1,1-trifluoroacetone. The synthesized ether-free Tmmp-Bmb-TFAc contains two piperidinium cations per polymer repeat unit in the main chain, which thus is employed as the AEM. The obtained AEM exhibits high ionic exchange capacity of 2.25 mmol g-1, low volume swelling of 13.6% and moderate tensile strength of 12.3 MPa in Br- form simultaneously. Meanwhile, the Tmmp-Bmb-TFAc membrane achieves a high conductivity of 45.0 mS cm-1 at 80 °C and possesses an excellent alk. stability in 1 mol L-1 KOH at 60°C within 480 h. Furthermore, no degradation of the polymer backbone is detected by 1H NMR spectra when immersing the membrane in 1 mol L-1 KOH at 80°C. This work provides a gentle and facile approach on the design and preparation of ether-free AEMs with cations in the polymer main chain. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Safety of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to bisalkylpiperidinium polymer preparation anion exchange membrane thermomech morphol property, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Safety of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 31, 2018, Rafiq, Kiran; Saify, Zafar Saied; Nesar, Shagufta; Faiyaz, Ambreen; Muhammad, Iyad Naeem published an article.HPLC of Formula: 574-98-1 The title of the article was Some novel piperidine analogues having strong alpha glucosidase inhibition. And the article contained the following:

In the present work some hydroxy piperidine analogs have been synthesized and analyzed for their hypoglycemic effect through glucosidase inhibition owing to the structural resemblance with nojirimycin. The activity was done by spectral absorbance anal. using acarbose as standard Two analogs 1-(1”-phenoxypropyl)-4-phenyl-4-hydroxy piperidinium hydrobromide and 1-(1”-adamantan acyl)-4-(4′-bromophenyl)-4-hydroxy piperidinium hydrobromide were found to pose excellent activity having 87.4 and 54.7% inhibition resp., hence strengthening the idea of studying piperidine analogs as glucosidase inhibitors due to structural similarity with nojirimycin. 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 piperidine derivative preparation alpha glucosidase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 2, 2020, Jang, Kyeongwoo; Horne, W. Seth; Asher, Sanford A. published an article.Application of 574-98-1 The title of the article was Human Serum Phenylpyruvate Quantification Using Responsive 2D Photonic Crystal Hydrogels via Chemoselective Oxime Ligation: Progress toward Developing Phenylalanine-Sensing Elements. And the article contained the following:

There is a need to develop at-home phenylalanine (Phe) test kits, analogous to home glucose meters, for phenylketonuria patients who must measure their blood Phe levels frequently to adjust their diet. Unfortunately, such test kits are not available yet because of the lack of simple and inexpensive Phe-sensing elements. With the goal of developing a Phe-sensing element, we fabricated two-dimensional photonic crystal (2DPC) hydrogels that quantify human serum phenylpyruvate (PhPY), which is the product of the reaction between Phe and the enzyme phenylalanine dehydrogenase. The PhPY-sensing hydrogels have oxyamine recognition groups that link PhPY to the hydrogel polymer network via chemoselective oxime ligation. This structural modification induces the hydrogel to swell, which then increases interparticle spacings within the embedded 2DPC. The PhPY-induced particle spacing changes are measured from light diffraction and used to quantify the PhPY concentrations The estimated limit of detection of PhPY in human serum for a detection time of 30 min is 19μM, which is comparable to the min. blood Phe concentrations of healthy people. Besides the potential application for developing Phe-sensing elements, this new hydrogel sensing approach via chemoselective oxime ligation is generalizable to the development of other chem. sensors working in complex biol. environments. 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 phenylpyruvate blood photonic crystal hydrogel phenylalanine sensing, oxime ligation, phenylalanine, phenylketonuria, photonic crystal, responsive hydrogel, Biochemical Methods: Spectral and Related Methods and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sun, Zhongwen; Chen, Lijun; Qiu, Kaixiong; Liu, Bo; Li, Hongtao; Yu, Fang published an article in 2022, the title of the article was Enantioselective Peroxidation of C-alkynyl imines enabled by chiral BINOL calcium phosphate.Application of 2567-29-5 And the article contains the following content:

Herein, a catalytic enantioselective addition of C-alkynyl imines, generated in-situ from N,O-acetals R1CCCH(OEt)NHR2 (R1 = Me3Si, Ph, 2-ClC6H4, 1-naphthyl, 2-thienyl, 3-pyridinyl, etc., R2 = Boc; R1 = Ph, R2 = Teoc, PhCO, Fmoc, Cbz) with hydroperoxides R3OOH (R3 = t-Bu, PhCH2, EtMe2, etc.) catalyzed by chiral BINOL calcium phosphate, affording a broad range of enantioenriched α-peroxy propargylamines (R)-R1CCCH(OOR3)NHR2 in good yields (80-99%) with high enantioselectivities (up to 94% ee) is reported. The protocol is characterized by mild conditions, easy accessibility and good practicability. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Application of 2567-29-5

The Article related to alkynyl amino peroxide asym synthesis, aminal alkynyl enantioselective peroxidation hydroperoxide binol calcium phosphate imine, Aliphatic Compounds: Peroxides and Hydroperoxides and other aspects.Application of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary