Month: December 2022

Adusumalli, Srinivasa Rao published the artcileAldehydes can switch the chemoselectivity of electrophiles in protein labeling, Application of 4-((6-Bromohexyl)oxy)-2-hydroxybenzaldehyde, the publication is Organic & Biomolecular Chemistry (2018), 16(48), 9377-9381, database is CAplus and MEDLINE.

We show that the chemoselectivity of an electrophile in protein labeling can be promiscuous. An aldehyde enables switching of chemoselectivity of an epoxide and a sulfonate ester along with an enhanced rate of reaction. The chem. technol. renders single-site installation of diverse probes on a protein and delivers anal. pure tagged proteins.

Organic & Biomolecular Chemistry published new progress about 1207448-58-5. 1207448-58-5 belongs to bromides-buliding-blocks, auxiliary class Bromide,Benzene,Phenol,Ether,Aldehyde, name is 4-((6-Bromohexyl)oxy)-2-hydroxybenzaldehyde, and the molecular formula is C13H17BrO3, Application of 4-((6-Bromohexyl)oxy)-2-hydroxybenzaldehyde.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Wu, Qiong published the artcilePoly[n]catenanes: Synthesis of molecular interlocked chains, Computed Properties of 1036461-93-4, the publication is Science (Washington, DC, United States) (2017), 358(6369), 1434-1439, database is CAplus and MEDLINE.

As the macromol. version of mech. interlocked mols., mech. interlocked polymers are promising candidates for the creation of sophisticated mol. machines and smart soft materials. Poly[n]catenanes, where the mol. chains consist solely of interlocked macrocycles, contain one of the highest concentrations of topol. bonds. We report, herein, a synthetic approach toward this distinctive polymer architecture in high yield (∼75%) via efficient ring closing of rationally designed metallosupramol. polymers. Light-scattering, mass spectrometric, and NMR characterization of fractionated samples support assignment of the high-molar mass product (number-average molar mass ∼21.4 kg per mol) to a mixture of linear poly[7-26]catenanes, branched poly[13-130]catenanes, and cyclic poly[4-7]catenanes. Increased hydrodynamic radius (in solution) and glass transition temperature (in bulk materials) were observed upon metalation with Zn²⁺.

Science (Washington, DC, United States) published new progress about 1036461-93-4. 1036461-93-4 belongs to bromides-buliding-blocks, auxiliary class Benzenes, name is 4-Bromo-N-butyl-2-nitroaniline, and the molecular formula is C15H24S, Computed Properties of 1036461-93-4.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Schwiderski, Ryan L. published the artcileSynthesis and Characterization of Thieno[3,4-b]pyrazine-Based Terthienyls: Tunable Precursors for Low Band Gap Conjugated Materials, Synthetic Route of 52431-30-8, the publication is Journal of Organic Chemistry (2013), 78(11), 5453-5462, database is CAplus and MEDLINE.

Synthetic methods have been developed for the preparation of new 2,3-dihalo- and 2,3-ditriflato-5,7-bis(2-thienyl)thieno[3,4-b]pyrazines. From these reactive intermediates, a variety of new 2,3-difunctionalized 5,7-bis(2-thienyl)thieno[3,4-b]pyrazines have been produced as precursors to conjugated materials. Structural, electronic, and optical characterization of these new analogs illustrate the extent to which the electronic nature of the functional groups can be used to tune the electronic properties of these thieno[3,4-b]pyrazine-based terthienyl units.

Journal of Organic Chemistry published new progress about 52431-30-8. 52431-30-8 belongs to bromides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 2,5-Dibromo-3,4-dinitrothiophene, and the molecular formula is C9H22OSi, Synthetic Route of 52431-30-8.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Ramu, Avner published the artcileReduced ouabain-sensitive potassium entry as a possible mechanism of multidrug-resistance in P388 cells, Application of Dimidium bromide, the publication is Biochemical Pharmacology (1991), 42(9), 1699-704, database is CAplus and MEDLINE.

Multidrug-resistant P388 cells were found to be resistant also to a variety of ammonium, phosphonium and arsonium compounds As previously shown for anthracyclines and vinca alkaloids, the resistance to the permanently charged lipophilic cationic compounds could be circumvented by verapamil. Relative to drug-sensitive cells, K⁺ uptake and plasma membrane Mg-ATPase activity in multidrug-resistant cells are ouabain resistant. The intracellular K⁺ concentration in drug-resistant cells is maintained at a normal level by increased activity of the furosemide sensitive transport system. It is suggested that the reduced activity of the electrogenic Na⁺-K⁺ pump in multidrug-resistant cells could result in a lower transmembrane potential and therefore reduced accumulation of cationic lipophilic compounds

Biochemical Pharmacology published new progress about 518-67-2. 518-67-2 belongs to bromides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Salt,Amine,Benzene, name is Dimidium bromide, and the molecular formula is C20H18BrN3, Application of Dimidium bromide.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Sankaranarayanan, Ananthakrishnan published the artcileNaphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure, Related Products of bromides-buliding-blocks, the publication is Molecular Pharmacology (2009), 75(2), 281-295, database is CAplus and MEDLINE.

Small-conductance (KCa2.1-2.3) and intermediate-conductance (KCa3.1) calcium-activated K⁺ channels are critically involved in modulating calcium-signaling cascades and membrane potential in both excitable and nonexcitable cells. Activators of these channels constitute useful pharmacol. tools and potential new drugs for the treatment of ataxia, epilepsy, and hypertension. Here, we used the neuroprotectant riluzole as a template for the design of KCa2/3 channel activators that are potent enough for in vivo studies. Of a library of 41 benzothiazoles, we identified 2 compounds, anthra[2,1-d]thiazol-2-ylamine (SKA-20) and naphtho[1,2-d]thiazol-2-ylamine (SKA-31), which are 10 to 20 times more potent than riluzole and activate KCa2.1 with EC₅₀ values of 430 nM and 2.9 μM, KCa2.2 with an EC₅₀ value of 1.9 μM, KCa2.3 with EC₅₀ values of 1.2 and 2.9 μM, and KCa3.1 with EC₅₀ values of 115 and 260 nM. Likewise, SKA-20 and SKA-31 activated native KCa2.3 and KCa3.1 channels in murine endothelial cells, and the more “drug-like” SKA-31 (half-life of 12 h) potentiated endothelium-derived hyperpolarizing factor-mediated dilations of carotid arteries from KCa3.1(+/+) mice but not from KCa3.1(-/-) mice. Administration of 10 and 30 mg/kg SKA-31 lowered mean arterial blood pressure by 4 and 6 mm Hg in normotensive mice and by 12 mm Hg in angiotensin-II-induced hypertension. These effects were absent in KCa3.1-deficient mice. In conclusion, with SKA-31, we have designed a new pharmacol. tool to define the functional role of the KCa2/3 channel activation in vivo. The blood pressure-lowering effect of SKA-31 suggests KCa3.1 channel activation as a new therapeutic principle for the treatment of hypertension.

Molecular Pharmacology published new progress about 111865-47-5. 111865-47-5 belongs to bromides-buliding-blocks, auxiliary class Benzenes, name is Mono(N,N,N-trimethyl-1-phenylmethanaminium) tribromide, and the molecular formula is C10H16Br3N, Related Products of bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Chung, Yun Mi published the artcilePhenol-containing bis(oxazolines): synthesis and fluorescence sensing of amines, Category: bromides-buliding-blocks, the publication is Tetrahedron (2006), 62(50), 11645-11651, database is CAplus.

The fluorescence sensing of primary amines as their neutral forms was studied with bis(oxazolinyl)phenols (Me-BOP, Ph-BOP), which are efficiently synthesized starting from mesitylene in six steps and in overall 12-22% yields. The BOP sensors showed fluorescence enhancement toward butylamine and several arylethylamines, whereas they showed fluorescence quenching toward secondary and branched amines. The opposite fluorescence behavior is explained by an increased conformational restriction at the excited state, at which a proton transfer complex between the host and guest forms that is stabilized in a tripodal hydrogen bonding mode. This is the 1st example in which fluorescence enhancement is observed in amine sensing with phenolic fluorophores. Enantiomeric α-chiral organoamines were also sensed with different fluorescent intensity changes by Ph-BOP, complementing the previous tris(oxazolines) that sense enantiomeric α-chiral organoammonium ions.

Tetrahedron published new progress about 111865-47-5. 111865-47-5 belongs to bromides-buliding-blocks, auxiliary class Benzenes, name is Mono(N,N,N-trimethyl-1-phenylmethanaminium) tribromide, and the molecular formula is C10H16Br3N, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Reddy, K. Rajendar published the artcileCetyltrimethylammonium Bromide as an Efficient Catalyst for Regioselective Bromination of Alkoxy Naphthalenes with Trimethyl Benzyl Ammonium Tribromide: Synthetic and Kinetic Approach, Application In Synthesis of 111865-47-5, the publication is International Journal of Chemical Kinetics (2014), 46(1), 10-23, database is CAplus.

Bromination of 2-alkoxynaphthalene (2-ANP) and its derivatives with trimethylbenzylammonium tribromide (TMBATB) did not proceed smoothly even under reflux conditions. But the addition of microconcns. of cetyltrimethyl ammonium bromide (CTAB) to the reaction afforded dramatic rate accelerations as well as good-to-excellent yield of the products ranging from 70% to 90%. Reactions underwent regioselective monobromination at 1-position of 2-alkoxynaphthalene. The rate of bromination has been followed conductometrically. The reaction kinetics indicated first-order kinetics in [2-ANP] as well as in [TMBATB]. Kinetic results in the presence of CTAB were explained on the basis of the Raghavan-Srinivasan model as applied to micelle-mediated bimol. reactions.

International Journal of Chemical Kinetics published new progress about 111865-47-5. 111865-47-5 belongs to bromides-buliding-blocks, auxiliary class Benzenes, name is Mono(N,N,N-trimethyl-1-phenylmethanaminium) tribromide, and the molecular formula is C10H16Br3N, Application In Synthesis of 111865-47-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Dunn, Derek published the artcileFrom an atypical wake-promoting agent to potent histamine-3 receptor inverse agonists, HPLC of Formula: 957061-13-1, the publication is Chemical Biology & Drug Design (2013), 81(3), 433-435, database is CAplus and MEDLINE.

Utilizing atypical wake-promoting agent modafinil (inactive in both rH₃ and hH₃ binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H₃ receptor inverse agonists were developed. A potent member of the series displayed excellent selectivity against related family members (H₁, H₂, and H₄ receptors).

Chemical Biology & Drug Design published new progress about 957061-13-1. 957061-13-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzene,Ether,Boronate Esters, name is 2-(4-(3-Bromopropoxy)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, and the molecular formula is C15H22BBrO3, HPLC of Formula: 957061-13-1.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Mistico, Laetitia published the artcileAccess to Silylated Pyrazole Derivatives by Palladium-Catalyzed C-H Activation of a TMS group, Formula: C7H8BBrO3, the publication is Chemistry – A European Journal (2016), 22(28), 9687-9692, database is CAplus and MEDLINE.

A simple and efficient approach to new silylated heterocycles of potential interest in medicinal chem. is presented. A set of bromophenyl trimethylsilyl pyrazole intermediates can be transformed by direct organometallic routes into two families of regioisomeric iodoaryl substrates; using either arylzinc or aryllithium chem., the TMS group remains on the pyrazole ring or translocates to the aryl moiety. These two families can then be efficiently transformed into benzo silino pyrazoles thanks to a single-step cyclization relying on the Pd-catalyzed activation of a nonactivated C(sp³)-H bond alpha to a Si atom. The exptl. conditions used, which are fully compatible with the pyrazole ring, suggest that this reaction evolves through a concerted metalation-deprotonation (CMD) mechanism.

Chemistry – A European Journal published new progress about 89694-44-0. 89694-44-0 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 2-Bromo-5-methoxybenzene boronic acid, and the molecular formula is C7H8BBrO3, Formula: C7H8BBrO3.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Xiao Long published the artcileSynthesis of the Major Metabolites of Febuxostat, Safety of 3-Bromo-2-methylpropanoic acid, the publication is Letters in Organic Chemistry (2015), 12(3), 217-221, database is CAplus.

Total synthesis of three Febuxostat metabolites, named 67M-1, 67M-2, and 67M-4,is described in this article. Through condensation of the key intermediate compound I with different side chains, and then oxidation and hydrolysis, we obtained three target compounds with an overall yield of 19.5%-28.0%.

Letters in Organic Chemistry published new progress about 56970-78-6. 56970-78-6 belongs to bromides-buliding-blocks, auxiliary class Bromide,Carboxylic acid,Aliphatic hydrocarbon chain,Inhibitor, name is 3-Bromo-2-methylpropanoic acid, and the molecular formula is C4H7BrO2, Safety of 3-Bromo-2-methylpropanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary