Month: November 2022

Baishya, Himankar published the artcileLyophilization cycle comparison and scale-up of esomeprazole sodium for injection between lab scale and scale-up batches vs FDM study, Quality Control of 161796-78-7, the publication is International Journal of Pharmaceutical Sciences and Research (2016), 7(11), 4407-4413, database is CAplus.

Lyophilization also known as freeze drying is a process in which water is removed from a product after it was frozen and placed under a vacuum, allowing the ice to change directly from solid to vapor without passing through a liquid phase. The process consists of three sep., unique, and interdependent processes; freezing, primary drying (sublimation), and secondary drying (desorption). Esomeprazole sodium for Injection 20 mg and 40 mg formulation was developed by optimized Lyophilization cycle. The objective of the research work was to compare the lyophilsation process cycle between Lab scale and scale up batches. The collapse temperature (Tc) for the product was identified using Freeze-drying microscope (FDM). During manufacturing the samples were exposed to above said collapse temperature to study the impact on product quality. Lab scale manufacturing was executed in Tofflon Lyophilizer 0.5 and scale-up batches were executed in Tofflon Lyophilizer 13. The Lyophilisation cycle and anal. results for both the batches were compared.

International Journal of Pharmaceutical Sciences and Research published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Quality Control of 161796-78-7.

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

Garcia, Andres published the artcileFabrication of bioconjugated and hybrid polymeric nanostructures by field-induced scanning probe lithography, Formula: C18H34N4O5S, the publication is Polymer Preprints (American Chemical Society, Division of Polymer Chemistry) (2007), 48(2), 11-12, database is CAplus.

Field-induced scanning probe lithog. (FISPL) was used to chem. modify polymer brushes directly to allow conjugation of biomols. Surface-confined non-fouling and protein resistant poly(oligo(ethylene glycol) Me methacrylate) (pOEGMA) brushes were prepared on silicon substrates by surface-initiated atom transfer radical polymerization (ATRP) in a grafting-from approach. These pOEGMA brushes were then patterned directly on the nanoscale by FISPL, generating chem. functionalities allowing for protein conjugation. gold was deposited onto silicon oxide patterns by field-emission from gold-coated AFM probes and this lithog. approach was used to pattern polymers and biomols. on silicon substrates. the unique nanofabrication approaches lead to nanostructures that can potentially be used as biosensors or as substrates for the precise presentation of biomol. queues to cells.

Polymer Preprints (American Chemical Society, Division of Polymer Chemistry) 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, Formula: C18H34N4O5S.

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

Liang, Shuang published the artcileHigh-performance chiral stationary phases based on chitosan derivatives with a branched-chain alkyl urea, Recommanded Product: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, the publication is Analytica Chimica Acta (2017), 183-193, database is CAplus and MEDLINE.

Two series of chitosan 3,6-bis(arylcarbamate)-2-(isobutylurea)s and corresponding coated-type chiral stationary phases (CSPs) were prepared from two kinds of chitosans with different mol. weights Most of the prepared CSPs demonstrated better enantioseparation performance than the homemade CSP of cellulose tris(3,5-dimethylphenylcarbamate). The CSPs of chitosan 3,6-bis(4-methylphenylcarbamate)-2-(isobutylurea) with higher mol. weight and chitosan 3,6-bis(3-chloro-4-methylphenylcarbamate)-2-(isobutylurea) with lower mol. weight possessed outstanding chiral recognition abilities which were at least as good as that of the commercialized CSP of Chiralcel OD-H towards the tested chiral analytes. Except for the two CSPs derived from chitosan 3,6-bis(4-methylphenylcarbamate)-2-(isobutylurea)s, the CSPs (the 1st class) with the chiral selectors of lower mol. weight provided better enantioseparations than the ones (the 2nd class) with the chiral selectors of higher mol. weight However, the chiral selectors of the 1st class CSPs showed higher swelling capacities in organic solvents than the ones of the 2nd class. All prepared CSPs could be analyzed with a wider range of mobile phases, in which some unusual organic solvents such as Et acetate, chloroform and THF etc. could be used as additives. According to separation performance and tolerance against organic solvents, the chitosan derivatives with branched-chain alkyl urea at 2-C of glucosamine residue were preferable to be used as chiral selectors for enantiomeric separation

Analytica Chimica Acta published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Recommanded Product: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide.

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

Zong, Guanghui published the artcileIpomoeassin F Binds Sec61α to Inhibit Protein Translocation, 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 Journal of the American Chemical Society (2019), 141(21), 8450-8461, database is CAplus and MEDLINE.

Ipomoeassin F is a potent natural cytotoxin that inhibits growth of many tumor cell lines with single-digit nanomolar potency. However, its biol. and pharmacol. properties have remained largely unexplored. Building upon our earlier achievements in total synthesis and medicinal chem., we used chem. proteomics to identify Sec61α (protein transport protein Sec61 subunit alpha isoform 1), the pore-forming subunit of the Sec61 protein translocon, as a direct binding partner of ipomoeassin F in living cells. The interaction is specific and strong enough to survive lysis conditions, enabling a biotin analog of ipomoeassin F to pull down Sec61α from live cells, yet it is also reversible, as judged by several experiments including fluorescent streptavidin staining, delayed competition in affinity pulldown, and inhibition of TNF biogenesis after washout. Sec61α forms the central subunit of the ER protein translocation complex, and the binding of ipomoeassin F results in a substantial, yet selective, inhibition of protein translocation in vitro and a broad ranging inhibition of protein secretion in live cells. Lastly, the unique resistance profile demonstrated by specific amino acid single-point mutations in Sec61α provides compelling evidence that Sec61α is the primary mol. target of ipomoeassin F and strongly suggests that the binding of this natural product to Sec61α is distinctive. Therefore, ipomoeassin F represents the first plant-derived, carbohydrate-based member of a novel structural class that offers new opportunities to explore Sec61α function and to further investigate its potential as a therapeutic target for drug discovery.

Journal of the American Chemical Society 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 C37H30ClIrOP2, 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

Zhao, Jin-Hui published the artcileNovel bluish green benzimidazole-based iridium(III) complexes for highly efficient phosphorescent organic light-emitting diodes, Formula: C19H14N2, the publication is New Journal of Chemistry (2017), 41(5), 1973-1979, database is CAplus.

Three multifluorinated benzimidazole-based iridium [Ir(III)] complexes abbreviated as 1F-Ir, 2F-Ir, and 3F-Ir were designed and synthesized. Their photoluminescent, thermal, and electrochem. properties were studied. These Ir(III) complexes exhibited strong bluish green emission with a high quantum efficiency of 0.68-0.81. Organic light-emitting diodes (OLEDs) with the simple structure of ITO/1,1-bis(4-(N,N-di(p-tolyl)amino)phenyl)cyclohexane (TAPC) (20 nm)/4,4′-N,N’-dicarbazole-biphenyl (CBP):Ir(III) complex (30 nm)/1,3,5-tris(N-phenylbenzimidazol-2-yl)benzene (TPBi) (50 nm)/8-hydroxyquinolinato lithium (Liq) (2 nm)/Al were fabricated to evaluate the potential applications of these fluorinated Ir(III) complexes. Good device performance (current efficiency: 48.0-70.1 cd A^-1 and external quantum efficiency: 15.6-21.7%) was achieved. In particular, OLEDs with 2F-Ir as a dopant emitter showed the best performance with a maximum current efficiency of 70.1 cd A^-1 and a maximum external quantum efficiency of 21.7% along with low efficiency roll-off. A very simple strategy has been reported to regulate the emitting color and improve the luminous efficiency of the Ir(III) phosphorescent emitters with great potential for practical applications in the field of OLEDs.

New Journal of 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 C10H10O2, Formula: C19H14N2.

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

Li, Jing published the artcileRepurposing of Antazoline Hydrochloride as an Inhibitor of Hepatitis B Virus DNA Secretion, Formula: C17H20ClN3, the publication is Virologica Sinica (2021), 36(3), 501-509, database is CAplus and MEDLINE.

Hepatitis B virus (HBV) belongs to Hepadnaviridae family and mainly infects hepatocytes, which can cause acute or chronic hepatitis. Currently, two types of antiviral drugs are approved for chronic infection clin.: interferons and nucleos(t)ide analogs. However, the clin. cure for chronic infection is still rare, and it is a huge challenge for all researchers to develop high-efficiency, safe, non-tolerant, and low-toxicity anti-HBV drugs. Antazoline hydrochloride is a first-generation antihistamine with anticholinergic properties, and it is commonly used to relieve nasal congestion and in eye drops. Recently, an in vitro high-throughput evaluation system was constructed to screen nearly 800 compounds from the Food and Drug Administration (FDA)-approved Drug Library. We found that arbidol hydrochloride and antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 4.321 μmol/L and 2.910 μmol/L in HepAD38 cells, resp. Moreover, the antiviral effects and potential mechanism of action of antazoline hydrochloride were studied in different HBV replication systems. The results indicate that antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells, with an EC₅₀ of 2.349 μmol/L. These findings provide new ideas for screening and research related to HBV agents.

Virologica Sinica 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, Formula: C17H20ClN3.

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

Wang, Yun published the artcileA Click Chemistry Mediated in Vivo Activity Probe for Dimethylarginine Dimethylaminohydrolase, SDS of cas: 359860-27-8, the publication is Journal of the American Chemical Society (2009), 131(42), 15096-15097, database is CAplus and MEDLINE.

Asym. N^ω,N^ω-dimethyl-L-arginine (ADMA) is an endogenously produced inhibitor of human nitric oxide synthase and an emerging biomarker for cardiovascular disease. Concentrations of ADMA are controlled by two isoforms of its catabolic enzyme dimethylarginine dimethylaminohydrolase (DDAH), the dysregulation of which has been studied as a mediating factor for endothelial dysfunction. A two-part, click-chem. mediated activity-based probe, N-but-3-ynyl-2-chloroacetamidine, is shown to label myc-tagged DDAH-1 expressed in HEK 293T cells, but not an inactive mutant or inhibited enzyme. A two-color Western blotting technique is used to determine the in vivo IC₅₀ value for a reversible inhibitor of DDAH-1, N⁵-(1-iminopropyl)-L-ornithine, indicating this compound’s bioavailability and its competition for binding to the active site. This probe provides a novel tool for the anal. of DDAH-1 activity in normal and pathophysiol. states and should allow more meaningful studies of the etiol. of endothelial dysfunction.

Journal of the American Chemical Society 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 C8H14O4, SDS of cas: 359860-27-8.

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

Zhao, Dongbing published the artcileRegiospecific Synthesis of 1,2-Disubstituted (Hetero)aryl Fused Imidazoles with Tunable Fluorescent Emission, Computed Properties of 2622-67-5, the publication is Organic Letters (2011), 13(24), 6516-6519, database is CAplus and MEDLINE.

A palladium-catalyzed two or fourfold amination was established that allows regiospecific synthesis of a diversity-oriented library of 1,2-disubstituted (hetero)aryl fused imidazoles, e.g., I, and provides an exceptional tool for the discovery of fluorescent scaffolds with tunable fluorescence emission. These fluorophores have been applied as fluorescent probes for live cell imaging.

Organic Letters 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 C8H7ClO3, Computed Properties of 2622-67-5.

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

Liu, Yan published the artcileCooperative modification of PVDF electroactive films due to the exfoliated and oriented Na ⁺– MMT with assistance of different cationic chain length ionic liquids, SDS of cas: 79917-90-1, the publication is Journal of Applied Polymer Science (2022), 139(22), 52238, database is CAplus.

Poly(vinylidene fluoride) (PVDF) based nano dielec. composites have been investigated widely due to their potential application in sensors, actuators, and energy storage fields. To achieve these goals, a novel modification of PVDF electroactive films was prepared due to the exfoliated and oriented Na⁺-MMT with the assistance of different cationic chain length imidazole-based ionic liquids The results proved the ion exchange between Na⁺-MMT and ILs promoted exfoliation and uniform dispersion of Na⁺-MMT in PVDF matrix efficiently even under a low ILs content (<0.05%). Furthermore, the existence of ILs and shearing force contributed to the oriented dispersion of Na⁺-MMT. The synergistic effect of Na⁺-MMT and ILs induced the crystal conformation transition from non-polar α-crystal to electroactive β/γ crystal. Compared with pure PVDF, PVDF/Na⁺-MMT/ILs nanocomposites with longer cationic chain ILs showed higher dielec. constant, breakdown strength, and energy d., while kept low-dielec. loss and conductivity The improved compatibility between PVDF and Na⁺-MMT due to the ion exchange and decreased crystal size for the polar β/γ crystal enhanced the transparency and elongation at break of PVDF/Na⁺-MMT/ILs nanocomposites significantly. The results proved [C16MIM][Cl] behaved optimum synergistic modification effect for the nanocomposites, and which showed potential applications in dielec. energy storage and microelectronic fields.

Journal of Applied Polymer Science published new progress about 79917-90-1. 79917-90-1 belongs to imidazoles-derivatives, auxiliary class Ionic Liquid,Ionic Liquid, name is 3-Butyl-1-methyl-1H-imidazol-3-ium chloride, and the molecular formula is C8H15ClN2, SDS of cas: 79917-90-1.

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

Mazars, Francois published the artcileSynthesis of Azolium-2-dithiocarboxylate Zwitterions under Mild, Aerobic Conditions, Quality Control of 258278-25-0, the publication is European Journal of Organic Chemistry (2021), 2021(13), 2025-2033, database is CAplus.

Twelve imidazolium-, imidazolinium-, or benzimidazolium-2-dithiocarboxylate zwitterions with aliphatic or aromatic substituents on their nitrogen atoms, including four new unsym. 1-alkyl-3-arylimidazolium derivatives, were obtained in high yields (62-96%) upon reaction of azolium salts with CS₂ and Cs₂CO₃ in acetonitrile at room temperature Compared to the previous strategies devised for the synthesis of NHC·CS₂ betaines, this novel procedure relied on an innocuous, weak base and could be applied under mild aerobic conditions. All the new compounds were fully characterized by various anal. techniques and the mol. structures of two of them were determined by XRD anal. An associative mechanism involving the concerted reaction of the azolium salts with both CS₂ and CO₃^2- was tentatively proposed to account for the formation of the zwitterionic adducts without the intervention of free carbenes. This would explain the good results obtained with a weak inorganic base that lacks the strength needed to deprotonate the azolium salt substrates.

European 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 C27H39ClN2, Quality Control of 258278-25-0.

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