Month: December 2022

Rose, Honor M. published the artcileDevelopment of an antibody-based, modular biosensor for ¹²⁹Xe NMR molecular imaging of cells at nanomolar concentrations, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, the publication is Proceedings of the National Academy of Sciences of the United States of America (2014), 111(32), 11697-11702, database is CAplus and MEDLINE.

Magnetic resonance imaging (MRI) is seriously limited when aiming for visualization of targeted contrast agents. Images are reconstructed from the weak diamagnetic properties of the sample and require an abundant mol. like water as the reporter. Micromolar to millimolar concentrations of conventional contrast agents are needed to generate image contrast, thus excluding many mol. markers as potential targets. To address this limitation, we developed and characterized a functional xenon NMR biosensor that can identify a specific cell surface marker by targeted 129Xe MRI. Cells expressing the cell surface protein CD14 can be spatially distinguished from control cells with incorporation of as little as 20 nM of the xenon MRI readout unit, cryptophane-A. Cryptophane-A serves as a chem. host for hyperpolarized nuclei and facilitates the sensitivity enhancement achieved by xenon MRI. Although this paper describes the application of a CD14-specific biosensor, the construct has been designed in a versatile, modular fashion. This allows for quick and easy adaptation of the biosensor to any cell surface target for which there is a specific antibody. In addition, the modular design facilitates the creation of a multifunctional probe that incorporates readout modules for different detection methods, such as fluorescence, to complement the primary MRI readout. This modular antibody-based approach not only offers a practical technique with which to screen targets, but one which can be readily applied as the xenon MRI field moves closer to mol. imaging applications in vivo.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C18H34N4O5S, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Sawlewicz, Jozef published the artcileSynthesis of thiocyanates derived from benzimidazole, Recommanded Product: (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, the publication is Acta Poloniae Pharmaceutica (1976), 33(4), 429-32, database is CAplus and MEDLINE.

2-(Hydroxymethyl)benzimidazole and ClCH2COCl in anhydrous dioxane yielded the benzimidazole I (R1 = R2 = H), which was treated with KSCN to give II (R1 = R2 = H). Analogously prepared were I and II (R1 and R2 given): H, Me; Me, H; PhCH2, H; PhCH2, Me. Chloroacetylation of the N-substituted benzimidazoles required an excess of ClCH2COCl to be used. The benzimidazoles were bactericidal.

Acta Poloniae Pharmaceutica published new progress about 7467-35-8. 7467-35-8 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Alcohol, name is (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, and the molecular formula is C9H10N2O, Recommanded Product: (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Guebitz, G. published the artcileThe TAS procedure in pharmaceutical analysis, HPLC of Formula: 2508-72-7, the publication is Scientia Pharmaceutica (1976), 44(1), 23-8, database is CAplus.

In the TAS (a thermomicro, thin-layer chromatog.) procedure, an unknown is mixed with a substance to facilitate its volatilization and heated in a special oven. The vapors are condensed on a chromatog. plate, separated, and identified. A table is given for 50 single and 6 combination pharmaceuticals listing the volatilizing substance, chromatog. solvent, method of visualization, and Rf factor.

Scientia Pharmaceutica published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, HPLC of Formula: 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Slade, Peter G. published the artcileProteins Modified by the Lipid Peroxidation Aldehyde 9,12-Dioxo-10(E)-dodecenoic Acid in MCF7 Breast Cancer Cells, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, the publication is Chemical Research in Toxicology (2010), 23(3), 557-567, database is CAplus and MEDLINE.

The hydroperoxide of linoleic acid (13-HPODE) degrades to 9,12-dioxo-10(E)-dodecenoic acid (DODE), which readily modifies proteins. This study identified the major proteins in MCF7 cells modified by DODE. To reduce false positives, three methods were used to identify DODE-modified proteins. First, cells were treated with a synthetically biotinylated 13-HPODE (13-HPODE-biotin). Modified proteins were enriched by NeutrAvidin affinity and identified by two-dimensional liquid chromatog.-tandem mass spectrometry (2D LC-MS/MS). Second, cells were treated with native 13-HPODE. Protein carbonyls were biotinylated with an aldehyde reactive probe, and modified proteins were enriched by NeutrAvidin affinity and identified by 2D LC-MS/MS. Third, using a newly developed DODE antibody, DODE-modified proteins were located by 2D SDS-PAGE and Western blot and identified by in-gel digestion and LC-MS/MS. Anal. of the proteins characterized by all three methods revealed a significant overlap and identified 32 primary proteins modified by DODE in MCF7 cells. These results demonstrated the feasibility for the cellular formation of DODE protein-carbonyl adducts that may be future indicators of oxidative stress.

Chemical Research in Toxicology published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C8H11NO, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Rojsitthisak, Pornchai published the artcileSimple HPLC determination of benzalkonium chloride in ophthalmic formulations containing antazoline and tetrahydrozoline, COA of Formula: C17H20ClN3, the publication is PDA Journal of Pharmaceutical Science and Technology (2005), 59(5), 332-337, database is CAplus and MEDLINE.

A simple and rapid anal. procedure for routine quantification of n-C₁₂H₂₅ and n-C₁₄H₂₉ benzalkonium chloride (C-12 and C-14 BKC) homologs in ophthalmic formulations containing antazoline HCl and tetrahydrozoline HCl by high-performance liquid chromatog. was developed and validated. The ophthalmic solution samples can be directly analyzed by reversed-phase on HiQ-Sil C18 column (4.6 mm × 150 mm, i.d., 5-μm particle size) with acetonitrile-sodium acetate buffer (pH 5.0; 0.2 M) (70:30, volume/volume) as mobile phase. UV Detection was carried out at 262 nm. The method was linear over the selected concentration and ranged from 0.03 to 0.10 mg/mL (r² = 0.9999) and from 0.01 to 0.05 mg/mL (r² = 0.9979) for C-12 and C-14 BKC homologs, resp. The mean percent recoveries were 100.2 and 102.6 and the percent CV values were 1.3 and 3.5 for C-12 and C-14 BKC homologs, resp. The results demonstrated the good linearity, accuracy, and precision. The method was applied to determine 2 com. ophthalmic formulations, and the percent label amounts of total BKC contents were found to be 99.7 and 103.2.

PDA Journal of Pharmaceutical Science and Technology published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, COA of Formula: C17H20ClN3.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Zhao, Rongrong published the artcileBis(2-methoxyethyl)ether promoted intramolecular acceptorless dehydrogenative coupling to construct structurally diverse quinazolinones by molecular oxygen, Safety of 1,2-Diphenyl-1H-benzo[d]imidazole, the publication is Green Chemistry (2022), 24(4), 1644-1649, database is CAplus.

A simple, efficient and clean approach for the synthesis of diverse dihydroisoquinolino[2,1-a]quinazolinones, 2-aryl quinazolinones and analogs through intramol. acceptorless dehydrogenative coupling has been achieved. The combination of bis(2-methoxyethyl)ether and mol. oxygen was identified as a highly efficient system for this oxidative dehydrogenative coupling sequential transformation without an external initiator, catalyst and additive. The applicability and practicability were demonstrated by a scope of twenty-nine examples and a gram-scale reaction. Some control experiments were also conducted to support a possible reaction pathway.

Green Chemistry published new progress about 2622-67-5. 2622-67-5 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Benzene,Benzimidazole, name is 1,2-Diphenyl-1H-benzo[d]imidazole, and the molecular formula is C18H34N4O5S, Safety of 1,2-Diphenyl-1H-benzo[d]imidazole.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Cui, Yang published the artcileDi-/trinuclear cationic Ir(III) complexes: Design, synthesis and application for highly sensitive and selective detection of TNP in aqueous solution, COA of Formula: C19H14N2, the publication is Sensors and Actuators, B: Chemical (2017), 314-322, database is CAplus.

Novel di- and trinuclear cationic iridium(III) complexes with flexible chain functionalized triazole-pyridine moieties as bridging ligands, namely DC-Ir and TC-Ir, were successfully synthesized and their photophys. and electrochem. properties studied. Despite DC-Ir and TC-Ir have different numbers of iridium(III) cores, the almost identical emissions in both solutions and aggregation states were observed Theor. calculations were performed to investigate their electronic structures and rationalize the photophys. and electrochem. behaviors. Compared with the emission in the solution, they exhibit enhanced photoluminescence in the aggregation states. Benefiting from the high emission in aqueous solution, DC-Ir and TC-Ir were employed as the “turn-off” sensors to detect the explosives. The results reveal that DC-Ir and TC-Ir show fast and highly sensitive and selective detection towards 2,4,6-trinitrophenol (TNP) owing to the efficient photo-induced electron transfer as well as the strong electrostatic interaction.

Sensors and Actuators, B: Chemical published new progress about 2622-67-5. 2622-67-5 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Benzene,Benzimidazole, name is 1,2-Diphenyl-1H-benzo[d]imidazole, and the molecular formula is C19H14N2, COA of Formula: C19H14N2.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Yanni, John M. published the artcileInhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Archives of Ophthalmology (Chicago) (1999), 117(5), 643-647, database is CAplus and MEDLINE.

To evaluate the effects of topical ocular drugs with histamine H₁-antagonist activity on histamine-stimulated phosphatidylinositol turnover and interleukin (IL) 6 and IL-8 secretion from human conjunctival epithelial cells. Primary human conjunctival epithelial cell cultures were stimulated with histamine in the presence or absence of test drugs. Phosphatidylinositol turnover was quantified by ion exchange chromatog. and cytokine content of supernatants by ELISA. Antazoline hydrochloride, emedastine difumarate, levocabastine hydrochloride, olopatadine hydrochloride, and pheniramine maleate attenuated histamine-stimulated phosphatidylinositol turnover and IL-6 and IL-8 secretion. Emedastine was the most potent in ligand binding, phosphatidylinositol turnover, and IL-6 secretion, with dissociation constant and 50% inhibitory concentrations of 1-3 nmol/L. Olopatadine, antazoline, and pheniramine exhibited similar H₁-binding affinities (32-39 nmol/L). However, olopatadine was approx. 10-fold more potent as an inhibitor of cytokine secretion (50% inhibitory concentration, 1.7-5.5 nmol/L) than predicted from binding data, while antazoline and pheniramine were far less potent (20- to 140-fold) in functional assays. Levocabastine (dissociation constant, 52.6 nmol/L) exhibited greater functional activity (50% inhibitory concentration, 8-25 nmol/L) than either antazoline or pheniramine. Histamine-stimulated phosphatidylinositol turnover and cytokine secretion by human conjunctival epithelial cells are attenuated by compounds with H₁-antagonist activity. However, antihistaminic potency alone does not predict anti-inflammatory potential. Olopatadine, emedastine, and levocabastine were notably more potent than pheniramine and antazoline. Selected topical ocular drugs with antihistaminic activity may offer therapeutic advantages to patients with allergic conjunctivitis by inhibiting proinflammatory cytokine secretion from human conjunctival epithelial cells.

Archives of Ophthalmology (Chicago) published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C20H28B2O4S2, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Wang, Lei published the artcileUnified Protocol for Fe-Based Catalyzed Biaryl Cross-Couplings between Various Aryl Electrophiles and Aryl Grignard Reagents, Related Products of imidazoles-derivatives, the publication is Journal of Organic Chemistry (2019), 84(9), 5176-5186, database is CAplus and MEDLINE.

The combination of commonly used FeCl₃/SIPr with Ti(OEt)₄/PhOM enabled a highly general iron-based catalyst system, which could efficiently catalyze the biaryl coupling reaction between various electrophiles (I, Br, Cl, OTs, OCONMe₂, OSO₂NMe₂) and common or functionalized aryl Grignard reagents with high functional group tolerance. Selective couplings of aryl iodides and bromides over the corresponding oxygen-based electrophiles have been achieved, and thus a terphenyl acid intermediate for anidulafungin was conveniently synthesized via an orthogonal coupling strategy.

Journal of Organic Chemistry published new progress about 258278-25-0. 258278-25-0 belongs to imidazoles-derivatives, auxiliary class Achiral NHCs Ligands, name is 1,3-Bis(2,6-diisopropylphenyl)-4,5-dihydro-1H-imidazol-3-ium chloride, and the molecular formula is C4H6F3NOS, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Deng, Yuchao published the artcileIron-Catalyzed Cross-Coupling of Alkynyl and Styrenyl Chlorides with Alkyl Grignard Reagents in Batch and Flow, HPLC of Formula: 258278-25-0, the publication is Chemistry – A European Journal (2019), 25(64), 14532-14535, database is CAplus and MEDLINE.

A selective, practical and fast iron-based cross-coupling reaction that enabled the formation of Csp-Csp³ and Csp²-Csp³ bonds. In a telescoped flow process, the reaction can be combined with the Grignard reagent synthesis. Moreover, flow allowed the use of a supporting ligand to be avoided without eroding the reaction selectivity.

Chemistry – A European Journal published new progress about 258278-25-0. 258278-25-0 belongs to imidazoles-derivatives, auxiliary class Achiral NHCs Ligands, name is 1,3-Bis(2,6-diisopropylphenyl)-4,5-dihydro-1H-imidazol-3-ium chloride, and the molecular formula is C27H39ClN2, HPLC of Formula: 258278-25-0.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem