Tag: M.W=250-300

Melancon, Bruce J. published the artcileIsatin replacements applied to the highly selective, muscarinic M₁ PAM ML137: Continued optimization of an MLPCN probe molecule, Product Details of C7H5Br2F, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(2), 412-416, database is CAplus and MEDLINE.

This Letter describes the continued optimization of an MLPCN probe mol. I (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M₁ PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M₁ receptor was also maintained.

Bioorganic & Medicinal Chemistry Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Product Details of C7H5Br2F.

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

Da Settimo, Federico published the artcile[1,2,4]Triazino[4,3-a]benzimidazole Acetic Acid Derivatives: A New Class of Selective Aldose Reductase Inhibitors, SDS of cas: 76283-09-5, the publication is Journal of Medicinal Chemistry (2001), 44(25), 4359-4369, database is CAplus and MEDLINE.

Acetic acid derivatives of [1,2,4]triazino[4,3-a]benzimidazole (TBI) were synthesized and tested in vitro and in vivo as a novel class of aldose reductase (ALR2) inhibitors. (10-Benzyl[1,2,4]triazino[4,3-a]benzimidazole-3,4(10H)-dion-2-yl)acetic acid (I), displayed the highest inhibitory activity (IC₅₀ = 0.36 μM) and effective in preventing cataract development in severely galactosemic rats when administered as an eyedrop solution All the compounds investigated were selective for ALR2, since none of them inhibited appreciably aldehyde reductase, sorbitol dehydrogenase, or glutathione reductase. The activity of I was lowered by inserting various substituents on the pendant Ph ring, by shifting the acetic acid moiety from the 2 to the 3 position of the TBI nucleus, or by cleaving the TBI system to yield benzimidazolylidenehydrazines as open-chain analogs. A three-dimensional model of human ALR2 was built, taking into account the conformational changes induced by the binding of inhibitors such as zopolrestat, to simulate the docking of I into the enzyme active site. The theor. binding mode of I was fully consistent with the structure-activity relationships in the TBI series and will guide the design of novel ALR2 inhibitors.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, SDS of cas: 76283-09-5.

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

Zuo, Minzan published the artcileMultiresponsive Supramolecular Theranostic Nanoplatform Based on Pillar[5]arene and Diphenylboronic Acid Derivatives for Integrated Glucose Sensing and Insulin Delivery, HPLC of Formula: 166821-88-1, the publication is Small (2018), 14(38), n/a, database is CAplus and MEDLINE.

A closed-loop “smart” insulin delivery system with the capability to mimic pancreatic cells will be highly desirable for diabetes treatment. This study reports a multiple stimuli-responsive insulin delivery platform based on an explicit supramol. strategy. Self-assembled from a well-designed amphiphilic host-guest complex formed by pillar[5]arene and a diphenylboronic acid derivative and loaded with insulin and glucose oxidase, the obtained insulin-GOx-loaded supramol. vesicles can selectively recognize glucose, accompanied by the structure disruption and efficient release of the entrapped insulin triggered by the high glucose concentration as well as the in situ generated H₂O₂ and acid microenvironment during the GOx-promoted specific oxidation of glucose into gluconic acid. Moreover, such a “smart” supramol. theranostic nanoplatform is able to function as both a glucose sensor and a controlled insulin delivery actuator. In vivo experiments further demonstrate that this smart supramol. nanocarrier shows fast response to hyperglycemic circumstances and can effectively regulate the glucose levels in a mouse model of type I diabetes.

Small published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C12H14IN, HPLC of Formula: 166821-88-1.

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

Deng, Mengyu published the artcileTricolor core/shell polymeric ratiometric nanosensors for intracellular glucose and oxygen dual sensing, Related Products of bromides-buliding-blocks, the publication is Sensors and Actuators, B: Chemical (2019), 437-444, database is CAplus.

Monitoring cell metabolism is crucial for understanding cell life activity and cytopathic mechanism. Glucose and oxygen are very important parameters for cell metabolism In this work, core/shell nanomaterials as novel tricolor ratiometric luminescence nanosensors were prepared for real-time monitoring of intracellular oxygen and glucose levels. The nanosensors were achieved by covalently embedding of red emitting oxygen probes and yellow emitting reference probes into the hydrophobic cores and covalently grafting blue emitting glucose probes onto hydrophilic shells. This system realized simultaneous detection of glucose and oxygen through two different luminescent signals without enzyme assistance, and the two kinds of detection signals didn′ t interfere with each other. The nanosensors could sensitively detect glucose in the range of 0.01 to 5.0 mM and simultaneously detect dissolved oxygen in the range of 0.05 to 39.3 mg/L, indicating the suitableness for intracellular glucose and oxygen monitoring. Because of the small sizes (< 60 nm), biocompatible core-shell structures, covalently imparted dye leaking-free construction of the nanosensors, these nanomaterials showed good cell permeability and low cytotoxicity. Cell imaging and intracellular sensing of the nanosensors were studied by confocal luminescence microscopy. Hela cells stained with the nanosensors showed an increase in blue emission when glucose was added and an increase in red emission when oxygen was reduced. While, the yellow emission from the reference probes was not affected by glucose or oxygen. This work is expected to lead to the design of intracellular glucose and oxygen sensors, and can be extended to other multiple sensors in biol. systems.

Sensors and Actuators, B: Chemical published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C12H16BBrO2, Related Products of bromides-buliding-blocks.

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

Doebelin, Christelle published the artcileIdentification of potent RORβ modulators: Scaffold variation, Name: (3-Bromo-5-isopropoxyphenyl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(19), 3210-3215, database is CAplus and MEDLINE.

The authors sought to develop RORβ-selective probe mols. to investigate the function of the receptor in vitro and in vivo and its role in the pathophysiol. of disease. To accomplish this, the authors modified a potent dual RORβ/RORγ inverse agonist from the primary literature with the goal of improving selectivity for RORβ vs. RORγ. Truncation of the Western portion of the mol. ablated activity at RORγ and led to a potent series of RORβ modulators. Continued exploration of this series investigated alternate replacement cores for the aminothiazole ring. Numerous suitable replacements were found during the course of the authors’ SAR investigations and are reported herein.

Bioorganic & Medicinal Chemistry Letters published new progress about 871125-81-4. 871125-81-4 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (3-Bromo-5-isopropoxyphenyl)boronic acid, and the molecular formula is C9H12BBrO3, Name: (3-Bromo-5-isopropoxyphenyl)boronic acid.

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

Malamas, Michael S. published the artcileDesign and Structure-Activity Relationships of Isothiocyanates as Potent and Selective N-Acylethanolamine-Hydrolyzing Acid Amidase Inhibitors, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5956-5972, database is CAplus and MEDLINE.

N-Acylethanolamines are signaling lipid mols. implicated in pathophysiol. conditions associated with inflammation and pain. N-Acylethanolamine acid amidase (NAAA) favorably hydrolyzes lipid palmitoylethanolamide, which plays a key role in the regulation of inflammatory and pain processes. The synthesis and structure-activity relationship studies encompassing the isothiocyanate pharmacophore have produced potent low nanomolar inhibitors for hNAAA, while exhibiting high selectivity (>100-fold) against other serine hydrolases and cysteine peptidases. We have followed a target-based structure-activity relationship approach, supported by computational methods and known cocrystals of hNAAA. We have identified systemically active inhibitors with good plasma stability (t_1/2 > 2 h) and microsomal stability (t_1/2 ∼ 15-30 min) as pharmacol. tools to investigate the role of NAAA in inflammation, pain, and drug addiction.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

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

Joly, D. published the artcileMetal-free organic sensitizers with narrow absorption in the visible for solar cells exceeding 10% efficiency, Formula: C12H19BrS, the publication is Energy & Environmental Science (2015), 8(7), 2010-2018, database is CAplus.

A novel family of six donor-acceptor type organic sensitizers for dye-sensitized solar cells (DSSCs) is reported. The dyes have been designed to have outstanding light absorption properties in the visible range and being able to achieve high photon-to-elec. current conversion for BIPV (building-integrated photovoltaic). Moreover, stability tests under illumination at 1 Sun and 65 °C showed a great stability for some of the devices, with less than 6% decrease of power conversion efficiency after 3000 h. The differences in the performance of the six sensitizers under standard illumination conditions can be correlated with the observed differences in the photo-induced transient photovoltage and in charge extraction measurements. We report the use of one of the dyes for the fabrication of semi-transparent solar modules showing an active area of 1400 cm² and a power output of 10.5 W m^-2.

Energy & Environmental Science published new progress about 303734-52-3. 303734-52-3 belongs to bromides-buliding-blocks, auxiliary class Thiophene,Bromide, name is 2-Bromo-3-(2-ethylhexyl)thiophene, and the molecular formula is C12H19BrS, Formula: C12H19BrS.

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

Luo, Qi published the artcileSynthesis of Metal-Containing Poly(thiophene methines) via Solid- and Melt-State Polymerization and Their Related Applications as Highly Sensitive Ni²⁺ Chemosensors, Name: 2-Bromo-3-(2-ethylhexyl)thiophene, the publication is Organometallics (2019), 38(3), 647-653, database is CAplus.

Metal-containing polymers have attracted continuous interest, for they combine the features of a metal complex and a polymer. Here, a series of thiophene methine based phenanthroline ligands (L1–L4) and their metal (Zn(II) and Cd(II)) complexes were prepared as monomers. Accordingly, metal-containing poly(thiophene methines) were prepared from these metal complexes via solid- and melt-state polymerization (S(M)SP). The polymerization process was preliminarily investigated by a crystal structure study, NMR anal., and absorbance spectra. Furthermore, the metal-free polymer (PL4) prepared directly from the ligand via MSP was tested as a metal ion chemosensor, which showed good selectivity and excellent sensitivity toward Ni²⁺ with a detection limit of 4.1 × 10^-9 M.

Organometallics published new progress about 303734-52-3. 303734-52-3 belongs to bromides-buliding-blocks, auxiliary class Thiophene,Bromide, name is 2-Bromo-3-(2-ethylhexyl)thiophene, and the molecular formula is C12H19BrS, Name: 2-Bromo-3-(2-ethylhexyl)thiophene.

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

Khedar, Poonam published the artcileClick chemistry inspired synthesis of piperazine-triazole derivatives and evaluation of their antimicrobial activities, HPLC of Formula: 76283-09-5, the publication is Medicinal Chemistry Research (2015), 24(7), 3117-3126, database is CAplus.

A series of novel piperazine-1,2,3-triazole derivatives I [R¹ = H, 4-F, 4-Cl, etc; R² = H, Cl, F; R³ = H, F, Cl, Br.], which entailed the bioisosteric replacement of the imidazole moiety and hybridization of two drug scaffolds was prepared by employing the regioselective copper (I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction. The synthesized compounds were evaluated for antibacterial activities against Gram-neg. (E. Coli and P. Putida), Gram-pos. S. Aureus bacteria and fungicidal activities against F. oxysporum, F. gramillarium and F. monalliforme fungi. Compound I [ R¹ = H, R² = Cl, R³ = F] exhibited moderate but promising antibacterial activity against Gram-neg. bacteria and fungicidal activity against F. oxysporum and F. gramillarium.

Medicinal Chemistry Research published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, HPLC of Formula: 76283-09-5.

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