imidazoles-derivatives Archives - Page 254 of 1008

Markovic, Nov’s team published research in Journal of Pharmaceutical and Biomedical Analysis in 42 | CAS: 161796-78-7

Journal of Pharmaceutical and Biomedical Analysis 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.

Markovic, Nov published the artcilePhysical and thermal characterization of chiral omeprazole sodium salts, Recommanded Product: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, the publication is Journal of Pharmaceutical and Biomedical Analysis (2006), 42(1), 25-31, database is CAplus and MEDLINE.

The phys. properties of drug substances may affect stability, manufacturing, dissolution and bioavailability. Variations in the degree of crystallinity in a pharmaceutical substance may exhibit physicochem. differences that impact at therapeutic, manufacturing, com. and legal levels, yet no reference has been found on the phys. properties of micronized omeprazole. This study reports on the phys. and thermal characterization of the sodium salts of S- and R-omeprazole, using diffuse reflectance IR Fourier transform spectroscopy (DRIFT), SEM, differential scanning calorimetry (DSC), microthermal anal. (μTA) and powder x-ray diffraction (XRPD). DSC experiments were performed in order to determine not only their thermal stability, but also the thermal history of both forms. SEM results indicate similar morphol., particle size and shape of powd. drug, while, μTA of processed disks shows different topog. images for S- and R-omeprazole, exhibiting a smoother surface for the S-form, indicative of the smoother particle size not evident in the SEM results. The low level of crystallinity of both enantiomers was confirmed by DRIFT spectroscopy and XRPD. Thermal stability by DSC of S- and R-omeprazole sodium salts was superior to that of the neutral omeprazole. This study has examined the phys. and thermal properties of both forms and in highlighting their differences provides an explanation for the potential differences in bioavailability and therapeutic efficacy.

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

Ali, Amir’s team published research in Acta Chimica Slovenica in 64 | CAS: 2508-72-7

Acta Chimica Slovenica 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, Quality Control of 2508-72-7.

Ali, Amir published the artcileStability indicating UHPLC-PDA assay for simultaneous determination of antazoline hydrochloride and naphazoline hydrochloride in ophthalmic formulations, Quality Control of 2508-72-7, the publication is Acta Chimica Slovenica (2017), 64(2), 332-341, database is CAplus and MEDLINE.

In the present study, a newly developed method based on ultrahigh performance liquid chromatog. (UHPLC) was optimized for the simultaneous determination of antazoline hydrochloride (ANZ) and naphazoline hydrochloride (NFZ) in ophthalmic formulations. Isocratic separation of ANZ and NFZ was performed at 40 °C with an ACE Excel 2 C18-PFP column (2 μm, 2.1 × 100 mm) at a flow rate of 0.6 mL min-1 whereas the mobile phase consisted of acetonitrile/phosphate buffer (60.40, volume/volume, pH 3.0) containing 0.5% triethylamine. Both analytes were detected at a wavelength of 285 nm and the injection volume was 1.0 μL. The overall run time per sample was 4.5 min with retention time of 0.92 and 1.86 min for NFZ and ANZ, resp. The calibration curve was linear from 0.500-100 μg mL-1 for ANZ and NFZ with a correlation coefficient ≥ 0.9981 while repeatability and reproducibility (expressed as relative standard deviation) were lower than 1.28 and 2.14%, resp. In comparison with high-performance liquid chromatog. (HPLC), the developed UHPLC method had remarkable advantages over HPLC as the run time was significantly reduced by 3.4-fold with a 5-fold decreased solvent consumption. Forced degradation studies indicated a complete separation of the analytes in the presence of their degradation products providing high degree of method specificity. The proposed UHPLC method was demonstrated to be simple and rapid for the determination of ANZ and NFZ in com. available ophthalmic formulations providing recoveries between 99.6 and 100.4%.

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

Gilchrist, M. Lane’s team published research in Analytical Chemistry (Washington, DC, United States) in 88 | CAS: 359860-27-8

Analytical Chemistry (Washington, DC, United States) 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.

Gilchrist, M. Lane published the artcileImaging and Functional Analysis of γ-Secretase and Substrate in a Proteolipobead System with an Activity-Based Probe, Formula: C18H34N4O5S, the publication is Analytical Chemistry (Washington, DC, United States) (2016), 88(2), 1303-1311, database is CAplus and MEDLINE.

Investigation of intramembranal protease catalysis demands the generation of intact biomembrane assemblies with structural integrity and lateral mobility. Here, we report the development of a microsphere supported-biomembrane platform enabling characterization of γ-secretase and substrate within proteolipobead assemblies via microscopy and flow cytometry. The active enzyme loading levels were tracked using an activity-based probe, with the biomembranes delineated by carbocyanine lipid reporters. Proteolipobeads formed from HeLa proteoliposomes gave rise to homogeneous distributions of active γ-secretase within supported biomembranes with native-like fluidity. The substrate loading into supported biomembranes was detergent-dependent, as evidenced by even colocalization of substrate and lipid tracers in confocal 3D imaging of individual proteolipobeads. Moreover, the loading level was tunable with bulk substrate concentration γ-Secretase substrate cleavage and its inhibition within γ-secretase proteolipobeads were observed This platform offers a means to visualize enzyme and substrate loading, activity, and inhibition in a controllable biomembrane microenvironment.

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

Gaber, Abd El-Aal M.’s team published research in Journal of Analytical and Applied Pyrolysis in 82 | CAS: 2622-67-5

Journal of Analytical and Applied Pyrolysis 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, Category: imidazoles-derivatives.

Gaber, Abd El-Aal M. published the artcileThermal fragmentation and rearrangement of N-arylbenzamidoxime and O-phenylsulfonyloxime derivatives, Category: imidazoles-derivatives, the publication is Journal of Analytical and Applied Pyrolysis (2008), 82(1), 110-116, database is CAplus.

Thermal fragmentation of N-arylbenzamide oximes I, II (Ar = Ph, p-tolyl) under nitrogen gives rise to benzanilide and 2-phenylbenzoxazole as the major products, in addition to benzonitrile, arylamines, phenols, benzoic acid, o- and p-aminophenols and benzimidazole derivatives In the presence of naphthalene as radical scavenger, I gave α- and β-naphthols beside the previous products. Also, heating N-arylbenzamide O-phenylsulfonyloximes III under reflux in boiling tetralin lead to the formation of benzonitrile, arylamines, diphenylamine, benzenesulfonic acid, di-Ph sulfone, 1-hydroxytetralin, α-tetralone, and 1,1′-bitetralyl as the major products. Analogous results are obtained on heating III in the presence of isoquinoline as a radical trap which formed 1-phenylisoquinoline. The isolated products have been interpreted in terms of a free radical mechanism involving the homolysis of N-O and/or C-N bonds.

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

Amodio, Emanuele’s team published research in Pediatrics in 2022-08-10 | CAS: 274-78-2

Pediatrics published new progress in MEDLINE about 274-78-2, 274-78-2 belongs to class imidazoles-derivatives, name is Imidazo[1,2-c]pyrimidine, and the molecular formula is C6H5N3, SDS of cas: 274-78-2.

Amodio, Emanuele published the artcileEffectiveness of mRNA COVID-19 Vaccines in Adolescents Over 6 Months., SDS of cas: 274-78-2, the main research area is .

BACKGROUND AND OBJECTIVES: On June 4, 2021, Italy launched the COVID-19 vaccination of adolescents to pace down the COVID-19 spread. Although clinical trials have evaluated mRNA vaccine effectiveness in adolescents, there is limited literature on its real-world effectiveness. Accordingly, this study aimed to estimate the effectiveness of mRNA COVID-19 vaccines against SARS-CoV-2 infection and mild or severe COVID-19 in a cohort of Sicilian adolescents within a six-month observation period. METHODS: A retrospective cohort study was conducted with adolescents aged 12-18, residents of Sicily, that were followed from July 15 to December 31, 2021. SARS-CoV-2 infections, mild and severe COVID-19, and COVID-19-related intubation or deaths during the study period were compared between subjects vaccinated with two doses of mRNA vaccines and unvaccinated individuals. The Cox regression analysis, adjusted for age and sex, was performed to compare the two groups. RESULTS: Overall, the study included a total at-risk population of 274,782 adolescents with 61.4% (168,633) of them having completed the vaccination cycle by the end of the study. Unvaccinated subjects had higher incidence rates of SARS-CoV-2 (1,043 x 10,000 vs. 158.7 x 10,000 subjects), mild COVID-19 (27.7 x 10,000 vs. 1.8 x 10,000 subjects) and severe COVID-19 (1.41 x 10,000 vs. 0 subjects) compared to the vaccinated population. The estimated adjusted vaccine effectiveness against SARS-CoV-2 infection was 71.2%, reaching 92.1% and 97.9% against mild and severe COVID-19, respectively. CONCLUSIONS: This study provides rigorous evidence of the mRNA COVID-19 vaccines effectiveness in protecting adolescents from both SARS-CoV-2 infection, and mild or severe COVID-19.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Louvanto, Karolina’s team published research in Acta obstetricia et gynecologica Scandinavica in 2010-12-07 | CAS: 1023-01-4

Acta obstetricia et gynecologica Scandinavica published new progress in MEDLINE about 1023-01-4, 1023-01-4 belongs to class imidazoles-derivatives, name is 2-(4-Bromophenyl)-6-methylimidazo[1,2-a]pyridine, and the molecular formula is C14H11BrN2, Computed Properties of 1023-01-4.

Louvanto, Karolina published the artcileHuman papillomavirus and predictors of cervical intraepithelial neoplasia among young mothers in a prospective follow-up study., Computed Properties of 1023-01-4, the main research area is .

OBJECTIVE: To study the incidence times and rates for cervical intraepithelial neoplasia (CIN) and its predictors. MATERIAL AND METHODS: This is a prospective follow-up study at Turku University Hospital, Finland. The Finnish Family human papillomavirus (HPV) study comprised 329 pregnant women followed up for 3 years. In an extension of the follow-up period, 171 women participated in an additional 3 years follow-up. Cervical scrapings for HPV testing and cervical smears were collected at each follow-up visit (2, 12, 24 and 36 months and 6 years). Following two abnormal cervical smears, colposcopy with biopsies was done. The main outcome measures were actuarial and crude incidence times, incidence rates and predictors of incident CIN. RESULTS: During the follow-up period, 10 women (3.2%) developed biopsy-confirmed CIN, and four presented with incident atypical squamous cells suggesting high-grade squamous intraepithelial lesion cytology. The CIN/squamous intraepithelial lesion developed in 74.5 and 66.3 months, with crude incidence rates of 13.4/1,000 and 15.1/1,000 women months at risk, respectively. In multivariate Poisson regression, independent predictors of incident CIN were as follows: high-risk HPV positive at baseline (incidence rate ratio = 5.54; 95% confidence interval 1.02-30.14, p= 0.048); type-specific high-risk HPV persistence during follow-up (incidence rate ratio = 5.84; 95% confidence interval 2.28-17.93, p= 0.0001); cervical smear cytologically diagnosed for atypical squamous cells of undetermined significance or worse at any follow-up visit (incidence rate ratio = 4.56; 95% confidence interval 2.37-8.78, p= 0.0001); and new sexual partner during follow-up (incidence rate ratio = 9.45; 95% confidence interval 1.90-46.97, p= 0.006). CONCLUSION: The results indicate that combined use of cervical smear and HPV testing, with prompt referral to colposcopy, enables accurate detection of incident CIN well before progression to invasive cancer. In addition to baseline and persistent high-risk HPV, abnormal cervical smear and new sexual partner are key predictors of incident CIN.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yeh, Herman J. C.’s team published research in Journal of the Chemical Society, Perkin Transactions 4: Physical Organic Chemistry in 1975 | CAS: 30086-17-0

Journal of the Chemical Society, Perkin Transactions 4: Physical Organic Chemistry published new progress about Ionization. 30086-17-0 belongs to class imidazoles-derivatives, name is 5-Fluoro-1H-imidazole, and the molecular formula is C3H3FN2, Safety of 5-Fluoro-1H-imidazole.

Yeh, Herman J. C. published the artcileFluorine-19 and proton nuclear magnetic resonance studies of ring-fluorinated imidazoles and histidines, Safety of 5-Fluoro-1H-imidazole, the main research area is imidazole fluoro NMR ionization; histidine fluoro NMR ionization; NMR fluoroimidazole fluorohistidine ionization.

1H and 19F titration curves in D2O and H2O, resp., were obtained for 2- and 4-fluoroimidazole and -histidine. Dissociation pK values were determined by computer-assisted curve fitting. Fluoroimidazoles are weaker bases and stronger acids than bromoimidazoles showing that the inductive effect of the halogen overshadows its resonance effect. Introduction of an alkyl group at C-5 displaces the F-4 and F-2 signals upfield and downfield, resp., indicating C-4 and C-5 are coupled by induction and resonance whereas C-2 and C-5 are coupled by induction only. Introduction of F displaces the H-2 and H-4 signals upfield. The shielding effect of the magnetic anisotropy of 19F counteracts the deshielding effect of its electronegativity. Protonation of the imidazole ring displaces the F-2 and F-4 signals downfield and upfield, resp., the same effect was observed in the imidazole anion. The amino acid side chain charge caused field perturbation of the 19F signal in fluorohistidines.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Melo, M. J.’s team published research in Zeitschrift fuer Naturforschung, B: Chemical Sciences in 1992-10-31 | CAS: 5805-53-8

Zeitschrift fuer Naturforschung, B: Chemical Sciences published new progress about Photolysis. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, COA of Formula: C9H8N2O2.

Melo, M. J. published the artcilePhotochemistry of 2-(2-furyl)benzimidazole (Fuberidazole), COA of Formula: C9H8N2O2, the main research area is photolysis furylbenzimidazole; benzimidazole furyl photolysis; Fuberidazole photolysis.

The photodegradation of 2-(2-furyl)benzimidazole (Fuberidazole) has been reinvestigated employing advanced HPLC-UV/VIS technique and fluorescence emission and excitation spectroscopy in methanol at natural pH, in acidic medium and in aqueous solutions at pH 7 and 3; four main products, benzimidazole-2-carboxylic acid, its Me ester, 1-methoxybenzimidazole, and Me 4-oxo-2-benzimidazolecrotonate (cis and trans isomers), besides benzimidazole and 2,2′-bibenzimidazole and other side products, have been isolated and characterized. The kinetics of the photodegradation process were followed independently by HPLC-UV and fluorescence emission and showed significant similarity; this allowed monitoring of a photodegradation at very low concentrations (5 × 10-5-5 × 10-6 M). The quantum yield of disappearance of Fuberidazole has been determined

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Robinson, Henry’s team published research in Chemistry – A European Journal in 2020-06-21 | CAS: 30086-17-0

Chemistry – A European Journal published new progress about Amination. 30086-17-0 belongs to class imidazoles-derivatives, name is 5-Fluoro-1H-imidazole, and the molecular formula is C3H3FN2, Synthetic Route of 30086-17-0.

Robinson, Henry published the artcileLate-Stage Functionalization by Chan-Lam Amination: Rapid Access to Potent and Selective Integrin Inhibitors, Synthetic Route of 30086-17-0, the main research area is naphthyridinylpentanamide arylpropanoic acid boronate Chan Lam amination; aminophenylpropanoic tetrahydro naphthyridinylpentanamide preparation integrin inhibitor idiopathic pulmonary fibrosis; C−N coupling; integrin antagonists; late-stage functionalization; medicinal chemistry; β-amino acids.

A late-stage functionalization of the aromatic ring in amino acid derivatives was described. The key step was a copper-catalyzed diversification of a boronate ester I (X = 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl; R1 = Boc; R2 = t-Bu) by amination (Chan-Lam reaction) that can be carried out on a complex β-aryl-β-amino acid scaffold. This not only considerably extended the substrate scope of amination partners, but also delivered an array of potent and selective integrin inhibitors I (X = 1-pyrazolyl, 4-chloro-1-imidazolyl, 1-piperidinyl, 1,4-oxazepan-4-yl, etc.; R1 = R2 = H) as potential treatment agents of idiopathic pulmonary fibrosis (IPF). This versatile chem. strategy, which was amenable to high-throughput-array protocols, allows the installation of pharmaceutically valuable heteroaromatic fragments at a late stage by direct coupling to NH heterocycles, leading to compounds with drug-like attributed.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wu, Qiongyou’s team published research in Heterocycles in 2004-03-01 | CAS: 21343-04-4

Heterocycles published new progress about Azidation. 21343-04-4 belongs to class imidazoles-derivatives, name is 5-Amino-1-methyl-1H-imidazole-4-carboxamide, and the molecular formula is C5H8N4O, Recommanded Product: 5-Amino-1-methyl-1H-imidazole-4-carboxamide.

Wu, Qiongyou published the artcileSynthesis and characterization of potential photolabeling probes for studying the antiviral mechanisms of EICAR, Recommanded Product: 5-Amino-1-methyl-1H-imidazole-4-carboxamide, the main research area is diazoniumribofuranosylimidazole azidoribofuranosylimidazole carboxamide nucleoside preparation azidolysis nucleophilic substitution photolysis.

The designed photo-labeling probes: 5-diazonium-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide (I) and 5-azido-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide (II) were synthesized via a short and convenient synthetic route, namely by diazotizing AICAR and subsequently performing substitution with NaN3. Although I was not stable even at low temperatures, II showed a rapid and clean photochem. reaction, which suggests that it may be a valuable tool for use in photo-labeling studies.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem