Category: 2567-29-5

On July 28, 2022, Grottelli, Silvia; Annunziato, Giannamaria; Pampalone, Gioena; Pieroni, Marco; Dindo, Mirco; Ferlenghi, Francesca; Costantino, Gabriele; Cellini, Barbara published an article.Recommanded Product: 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Identification of Human Alanine-Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1. And the article contained the following:

Primary hyperoxaluria type I (PH1) is a rare kidney disease due to the deficit of alanine:glyoxylate aminotransferase (AGT), a pyridoxal-5′-phosphate-dependent enzyme responsible for liver glyoxylate detoxification, which in turn prevents oxalate formation and precipitation as kidney stones. Many PH1-associated missense mutations cause AGT misfolding. Therefore, the use of pharmacol. chaperones (PCs), small mols. that promote correct folding, represents a useful therapeutic option. To identify ligands acting as PCs for AGT, we first performed a small screening of com. available compounds We tested each mol. by a dual approach aimed at defining the inhibition potency on purified proteins and the chaperone activity in cells expressing a misfolded variant associated with PH1. We then performed a chem. optimization campaign and tested the resulting synthetic mols. using the same approach. Overall, the results allowed us to identify a promising hit compound for AGT and draw conclusions about the requirements for optimal PC activity. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Recommanded Product: 4-(Bromomethyl)-1,1′-biphenyl

The Article related to alanine glyoxylate aminotransferase ligand preparation chaperone primary hyperoxaluria, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 7, 2022, Zhang, Qiao; Wang, Simin; Zhang, Qian; Xiong, Tao published an article.HPLC of Formula: 2567-29-5 The title of the article was Radical Addition-Triggered Remote Migratory Isomerization of Unactivated Alkenes to Difluoromethylene-Containing Alkenes Enabled by Bimetallic Catalysis. And the article contained the following:

A fascinating alkene remote migratory isomerization engendered by carbon radical addition to C=C bond in alkenes Ar(CH2)nCH=CH2 (Ar = C6H5, 4-FC6H4, 2-pyridyl, etc.; n = 2, 4, 5, 6, 7) via bimetallic catalysis has been disclosed. A diverse array of alkenes bearing distantly incorporated the difluoromethylene ArCH=CH(CH2)mCF2C(O)R (m = 1, 4, 5, 6, 9; R = OMe, OEt, morpholin-4-yl, etc.) functionality have been expediently obtained. The retainment of C=C bonds in products could serve as an useful synthetic platform furnishing otherwise difficult to access value-added densely functionalized difluoromethylene containing mols. In addition, some exptl. studies have been implemented to shed light on the probable mechanism. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).HPLC of Formula: 2567-29-5

The Article related to difluoromethyl alkene preparation diastereoselective, alkene radical addition isomerization, Aliphatic Compounds: Hydrocarbons and other aspects.HPLC of Formula: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 4, 2022, Matsumoto, Akira; Yamamoto, Masanori; Maruoka, Keiji published an article.Formula: C13H11Br The title of the article was Cationic DABCO-Based Catalyst for Site-Selective C-H Alkylation via Photoinduced Hydrogen-Atom Transfer. And the article contained the following:

A series of hydrogen-atom transfer (HAT) catalysts based on the readily available and tunable 1,4-diazabicyclo[2.2.2]octane (DABCO) structure was designed, and their photoinduced HAT catalysis ability was demonstrated. The combination of HAT catalyst with an acridinium-based organophotoredox catalyst enabled efficient and site-selective C-H alkylation of substrates ranging from unactivated hydrocarbons to complex mols. Notably, a HAT catalyst with addnl. substituents adjacent to a nitrogen atom further improved the site selectivity. Mechanistic studies suggested that the N-substituent of the catalyst played a crucial role, assisting in the generation of a dicationic aminium radical as an active species for the HAT process. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Formula: C13H11Br

The Article related to alkene alkane dabco acridinium catalyst photochem alkylation regioselective, alkane preparation, Aliphatic Compounds: Hydrocarbons and other aspects.Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 14, 2022, Huang, Jian; Shi, Qiong; Choudhry, Namrta; Li, Hongmei; Yang, Chenglu; Kalashova, Julia; Yan, Ziqi; Li, Jinhua; Reddy, Mallu Chenna; Gopala, Sridhar Goud; Zhang, Shenqiu; Zhang, Jing; Nimishetti, Naganna; Yang, Dun published an article.HPLC of Formula: 2567-29-5 The title of the article was Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. And the article contained the following:

We used mechanism-informed phenotypic screening to identify and optimize compounds that phenocopy the genetic depletion of the mitotic aurora kinase B (AURKB) kinase. After assaying nine aryl fused seven-membered lactam compounds, we identified a hit compound 6a that was subsequently optimized to five lead compounds with low nanomolar activity, represented by the lead compound 6v (19 nM). With excellent drug-like properties, these compounds reproduced the loss of function in phenotypes of AURKB and exhibited potent cytotoxic activities in various cancer cell lines. Collectively, these data support that seven-membered lactam-based analogs might be valuable for further development as a new type of antimitotic agents for the treatment of cancer. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).HPLC of Formula: 2567-29-5

The Article related to lactam compound prepnd aurora kinase b inhibitor cancer, Placeholder for records without volume info and other aspects.HPLC of Formula: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Rothschild, Daniel A.; Kopcha, William P.; Tran, Aaron; Zhang, Jianyuan; Lipke, Mark C. published an article in 2022, the title of the article was Gram-scale synthesis of a covalent nanocage that preserves the redox properties of encapsulated fullerenes.SDS of cas: 2567-29-5 And the article contains the following content:

Discrete nanocages provide a way to solubilize, sep., and tune the properties of fullerenes, but these 3D receptors cannot usually be synthesized easily from inexpensive starting materials, limiting their utility. Herein, we describe the first fullerene-binding nanocage (Cage4+) that can be made efficiently on a gram scale. Cage4+ was prepared in up to 57% yield by the formation of pyridinium linkages between complemantary porphyrin components that are themselves readily accessible. Cage4+ binds C60 and C70 with large association constants (>108 M-1), thereby solubilizing these fullerenes in polar solvents. Fullerene association and redox-properties were subsequently investigated across multiple charge states of the host-guest complexes. Remarkably, neutral and singly reduced fullerenes bind with similar strengths, leaving their 0/1- redox couples minimally perturbed and fully reversible, whereas other hosts substantially alter the redox properties of fullerenes. Thus, C60@Cage4+ and C70@Cage4+ may be useful as solubilized fullerene derivatives that preserve the inherent electron-accepting and electron-transfer capabilities of the fullerenes. Fulleride dianions were also found to bind strongly in Cage4+, while further reduction is centered on the host, leading to lowered association of the fulleride guest in the case of C602-. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).SDS of cas: 2567-29-5

The Article related to covalent nanocage preserve redox property encapsulated fullerene, Placeholder for records without volume info and other aspects.SDS of cas: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 24, 2020, Ang, Chee Wei; Tan, Lendl; Sykes, Melissa L.; AbuGharbiyeh, Neda; Debnath, Anjan; Reid, Janet C.; West, Nicholas P.; Avery, Vicky M.; Cooper, Matthew A.; Blaskovich, Mark A. T. published an article.SDS of cas: 2567-29-5 The title of the article was Antitubercular and Antiparasitic 2-Nitroimidazopyrazinones with Improved Potency and Solubility. And the article contained the following:

Following the approval of delamanid and pretomanid as new drugs to treat drug-resistant tuberculosis, there is now a renewed interest in bicyclic nitroimidazole scaffolds as a source of therapeutics against infectious diseases. We recently described a nitroimidazopyrazinone bicyclic subclass with promising antitubercular and antiparasitic activity, prompting addnl. efforts to generate analogs with improved solubility and enhanced potency. The key pendant aryl substituent was modified by (i) introducing polar functionality to the methylene linker, (ii) replacing the terminal Ph group with less lipophilic heterocycles, or (iii) generating extended biaryl side chains. Improved antitubercular and antitrypanosomal activity was observed with the biaryl side chains, with most analogs achieved 2- to 175-fold higher activity than the monoaryl parent compounds, with encouraging improvements in solubility when pyridyl groups were incorporated. This study has contributed to understanding the existing structure-activity relationship (SAR) of the nitroimidazopyrazinone scaffold against a panel of disease-causing organisms to support future lead optimization. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).SDS of cas: 2567-29-5

The Article related to structure antitubercular antiparasitic nitroimidazo pyrazinone derivative preparation, Placeholder for records without volume info and other aspects.SDS of cas: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 31, 2020, Kickinger, Stefanie; Al-Khawaja, Anas; Haugaard, Anne Staehr; Lie, Maria E. K.; Bavo, Francesco; Loeffler, Rebekka; Damgaard, Maria; Ecker, Gerhard F.; Froelund, Bente; Wellendorph, Petrine published an article.COA of Formula: C13H11Br The title of the article was Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors. And the article contained the following:

We have previously identified 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid (ATPCA) as the most potent substrate-inhibitor of the betaine/GABA transporter 1 (BGT1) (IC50 2.5 μM) reported to date. Herein, we characterize the binding mode of 20 novel analogs and propose the mol. determinants driving BGT1-selectivity. A series of N1-, exocyclic-N-, and C4-substituted analogs was synthesized and pharmacol. characterized in radioligand-based uptake assays at the four human GABA transporters (hGATs) recombinantly expressed in mammalian cells. Overall, the analogs retained subtype-selectivity for hBGT1, though with lower inhibitory activities (mid to high micromolar IC50 values) compared to ATPCA. Further characterization of five of these BGT1-active analogs in a fluorescence-based FMP assay revealed that the compounds are substrates for hBGT1, suggesting they interact with the orthosteric site of the transporter. In silico-guided mutagenesis experiments showed that the non-conserved residues Q299 and E52 in hBGT1 as well as the conformational flexibility of the compounds potentially contribute to the subtype-selectivity of ATPCA and its analogs. Overall, this study provides new insights into the mol. interactions governing the subtype-selectivity of BGT1 substrate-inhibitors. The findings may guide the rational design of BGT1-selective pharmacol. tool compounds for future drug discovery. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).COA of Formula: C13H11Br

The Article related to amino tetrahydropyrimidine carboxylic acid betaine gaba transporter substrate inhibitor, Placeholder for records without volume info and other aspects.COA of Formula: C13H11Br

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 November 5, 2021, Grollier, Kevin; Chefdeville, Emmanuel; De Zordo-Banliat, Arnaud; Pegot, Bruce; Dagousset, Guillaume; Magnier, Emmanuel; Billard, Thierry published an article.HPLC of Formula: 2567-29-5 The title of the article was Fe-mediated nucleophilic trifluoromethylselenolation of activated alkyl bromides via umpolung reactivity of trifluoromethyl tolueneselenosulfinate. And the article contained the following:

Trifluoromethyl tolueneselenosulfonate is a versatile reagent which can be reduced by iron powder to generate in situ trifluoromethylselenolate anion which can then react with alkyl bromide to form (trifluoromethyl)selanes RSeCF3 [R = Bn, CH2Bn, CH2C(O)Ph, etc.] through SN2 reaction. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).HPLC of Formula: 2567-29-5

The Article related to trifluoromethyl selane preparation, alkyl bromide trifluoromethyl tolueneselenosulfinate trifluoromethylselenolation iron powder, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 17, 2021, Zhang, Min; Lin, Jin-Hong; Xiao, Ji-Chang published an article.Synthetic Route of 2567-29-5 The title of the article was HCF2Se/HCF2S Installation by Tandem Substitutions from Alkyl Bromides. And the article contained the following:

Herein authors describe an efficient construction of HCF2Se and HCF2S groups by tandem substitutions between alkyl bromides and a reagent system consisting of MSeCN (or MSCN) and Ph3P+CF2H Br-. The tandem process occurs via the first nucleophilic substitution of alkyl bromides by -SeCN (or -SCN) and the subsequent nucleophilic difluoromethylation. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Synthetic Route of 2567-29-5

The Article related to difluoromethylseleno difluoromethylthio preparation, alkyl bromides difluoromethylselenolation difluoromethylthiolation, General Organic Chemistry: Synthetic Methods and other aspects.Synthetic Route of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary