Tag: M.W=300-350

Yin, Jinjin published the artcileNifedipine or amlodipine? The choice for hypertension during pregnancy: a systematic review and meta-analysis, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Archives of Gynecology and Obstetrics, database is CAplus and MEDLINE.

There is a lack of sufficient evidence regarding efficacy and safety of amlodipine on treating hypertension during pregnancy. To compare antihypertensive efficacy, pregnancy outcome and safety of amlodipine with nifedipine on hypertension during pregnancy. A systematic search of PubMed, Embase, Cochrane Library, clinicaltrials.gov, Chinese National Knowledge Infrastructure, Wanfang Database and China Biol. Medicine disk of randomized controlled trials (RCTs) up to Apr. l5, 2021 was conducted on RCTs comparing amlodipine to nifedipine for the treatment of hypertension during pregnancy. Screening, data extraction, and quality assessment were done by two independent reviewers. To estimate relative effects from all available evidence, a meta-anal. was conducted. Seventeen RCTs were included. Amlodipine was found the efficacy is slightly superior to nifedipine on treating hypertension during pregnancy (RR 1.06, 95% CI 1.01 to 1.10) with a decreased risk for maternal side effects (RR 0.42, 95% CI 0.29 to 0.61). Subgroup anal. found amlodipine can get a better control on SBP (RR – 11.68, 95% CI – 17.98 to – 5.37) and DBP (RR – 7.44, 95% CI – 13.81 to – 1.06) compared with intermediate-/long-acting nifedipine. In addition, there was no difference between amlodipine and nifedipine on pregnancy outcomes including caesarean section, premature labour, placental abruption, FGR, fetal distress, neonatal asphyxia. Given the results of this systematic review and meta-anal., amlodipine can be effectively and safely used for hypertension during pregnancy.

Archives of Gynecology and Obstetrics published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C5H10O, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Souza de Araujo, Guilherme Rodolfo published the artcileMicroemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: Structural and in vitro study, Application In Synthesis of 21829-25-4, the publication is Colloids and Surfaces, B: Biointerfaces (2022), 112474, database is CAplus and MEDLINE.

Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility This study aimed to develop a microemulsified system with low surfactant concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index < 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers, acting by rising the coefficients of partition and diffusion of the nifedipine in the skin.

Colloids and Surfaces, B: Biointerfaces published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C15H14N2, Application In Synthesis of 21829-25-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Nishide, Shigenori published the artcileImproved determination of betahistine mesylate, Synthetic Route of 54856-23-4, the publication is Yakugaku Zasshi (1983), 103(11), 1180-4, database is CAplus and MEDLINE.

An improved method for the determination of betahistine mesylate (I) [54856-23-4] in tablets was developed by the use of UV spectrophotometry at 260 nm. The determination of in aqueous solutions were affected by pH and temperature The measurement of the mesylate in 0.1 N sulfuric acid instead of water produced more accurate results.

Yakugaku Zasshi published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C10H20N2O6S2, Synthetic Route of 54856-23-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Michiba, Kazuyoshi published the artcileUsefulness of human jejunal spheroid-derived differentiated intestinal epithelial cells for the prediction of intestinal drug absorption in humans, Product Details of C17H18N2O6, the publication is Drug Metabolism & Disposition (2022), 50(3), 204-213, database is CAplus and MEDLINE.

This study aimed to demonstrate the usefulness of human jejunal spheroid-derived differentiated intestinal epithelial cells as a novel in vitro model for clarifying the impact of intestinal drug-metabolizing enzymes and transporters on the intestinal absorption of substrate drugs in humans. Three-dimensional human intestinal spheroids were successfully established from surgical human jejunal specimens and expanded for a long period using L-WRN-conditioned medium, which contains Wnt3a, R-spondin 3, and noggin. The mRNA expression levels of intestinal pharmacokinetics-related genes in the human jejunal spheroid-derived differentiated intestinal epithelial cells were drastically increased over a 5-day period after seeding compared with those in human jejunal spheroids and were approx. the same as those in human jejunal tissue over a culture period of at least 13 days. Activities of typical drug-metabolizing enzymes [cytochrome P 450 (CYP) 3A, CYP2C9, uridine 5-diphospho-glucuronosyltransferase 1A, and carboxylesterase 2] and uptake/efflux transporters [peptide transporter 1/solute carrier 15A1], P-glycoprotein, and breast cancer resistance protein) in the differentiated cells were confirmed. Furthermore, intestinal availability (Fg) values estimated from the apical-to-basolateral permeation clearance across cell monolayer showed a good correlation with the in vivo Fg values in humans for five CYP3A substrate drugs (Fg range, 0.35-0.98). In conclusion, the functions of major intestinal drug-metabolizing enzymes and transporters could be maintained in human jejunal spheroid-derived differentiated intestinal epithelial cells. This model would be useful for the quant. evaluation of the impact of intestinal drug-metabolizing enzymes and transporters on the intestinal absorption of substrate drugs in humans.

Drug Metabolism & Disposition published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lee, Yao published the artcileViral replication and innate immunity of feline herpesvirus-1 virulence-associated genes in feline respiratory epithelial cells, Category: pyridine-derivatives, the publication is Virus Research (2019), 56-67, database is CAplus and MEDLINE.

Feline herpesvirus-1 (FHV-1) infection occurs worldwide and is a leading cause of respiratory and ocular diseases in cats. Current vaccines reduce the severity of symptoms but do not prevent infection and, therefore, do not provide defense against an establishment of latency and reactivation. We hypothesize that immunomodulation of FHV-1 is the cause of lack in protection and that deletion of virulence/immune modulatory genes of FHV-1 will enhance safety and immunogenicity. Our objective was to use feline respiratory epithelial cell (FREC) cultures to define in vitro growth characteristics and immunomodulation resulting from infection of FRECs with the virulent FHV-1 strain C27 (WT) and glycoprotein C-deletion (gC-), glycoprotein E-deletion (gE-), serine/threonine protein kinase-deletion (PK-), as well as gE and thymidine kinase-double-deletion (gE-TK-) mutants generated by bacterial artificial chromosome mutagenesis. Differentiated FRECs were mock inoculated or inoculated with WT, gC-, gE-, PK-, or gE-TK- mutants. Virus titration and real-time quant. PCR assays were performed on samples collected at 1 hpi followed by 24 h intervals between 24 and 96 hpi to determine growth kinetics. Real-time PCR was used to quantitate IFNa, TNFa, IL-1β, IL-10, and TGFβ-specific mRNA levels. Immunoassays were performed to measure the protein levels of subsets of cytokines/chemokines secreted by FRECs. Inoculation of FRECs with gE-TK- resulted in significantly lower end-point titers than inoculation with WT or gE-. Both PK- and gC- inoculated FRECs also produced significantly lower end-point titers at 96 hpi than WT. Overall, intracellular virus titers were higher than those of extracellular virus. PCR results for viral DNA paralleled the virus titration results. Further, in contrast to WT inoculation, an increase in IFNa and IL-10 mRNA expression was not observed following inoculation with gE-TK- and PK-, but inoculation with gE-TK- and PK- did result in increased TGFβ expression in FRECs compared to responses following infection with WT. Moreover, gE-TK- and PK- blocked the inhibition of IL-8 and neutrophil chemoattractant (KC), which was observed following inoculation with WT. In summary, the results obtained in FRECs may be used to predict the safety and immunogenicity characteristics of these mutants in vivo. Our study highlights the value of the FREC system for studying replication kinetics/immune modulation factors of FHV-1 and screening prospective vaccine candidates before their use in exptl. cats.

Virus Research published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zhang, Xudong published the artcileHergSPred: Accurate Classification of hERG Blockers/Nonblockers with Machine-Learning Models, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Chemical Information and Modeling (2022), 62(8), 1830-1839, database is CAplus and MEDLINE.

The human ether-á-go-go-related gene (hERG) K+ channel plays an important role in cardiac action potentials. The inhibition of the hERG channel may lead to long QT syndrome (LQTS) and even sudden cardiac death. Due to severe hERG-related cardiotoxicity, many drugs have been withdrawn from the market. Therefore, it is necessary to estimate the chem. blockade of hERG in the early stage of drug discovery. In this study, we collected 12,850 compounds with hERG inhibition data from the literature and trained a series of hERG blocking classification models based on the MACCS and Morgan fingerprints. A consensus model named HergSPred was generated based on the individual models using voting principles. The accuracy of HergSPred is higher than previous models using identical training and test sets. Moreover, we analyzed the contribution of each input fingerprint to the prediction output to obtain intuitive chem. insights into the hERG inhibition, which allows visualization of warning substructures that may cause cardiotoxicity in the input compound The model is available at http://www.icdrug.com/ICDrug/T.

Journal of Chemical Information and Modeling published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H37NO3, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lauro, Figueroa-Valverde published the artcileSynthesis and Biological Activity of the Pyridine-hexacyclic-steroid Derivative on a Heart Failure Model., Computed Properties of 21829-25-4, the publication is Anti-inflammatory & anti-allergy agents in medicinal chemistry (2022), 21(1), 34-45, database is MEDLINE.

BACKGROUND: Several drugs with inotropic activity have been synthesized; however, there is very little information on biological activity exerted by steroid derivatives in the cardiovascular system. OBJECTIVE: The aim of this research was to prepare a steroid-pyridine derivative to evaluate the effect it exerts on left ventricular pressure and characterize its molecular interaction. METHODS: The first stage was carried out through the synthesis of a steroid-pyridine derivative using some chemical strategies. The second stage involved the evaluation of the biological activity of the steroid-pyridine derivative on left ventricular pressure using a model of heart failure in the absence or presence of the drugs, such as flutamide, tamoxifen, prazosin, metoprolol, indomethacin, and nifedipine. RESULTS: The results showed that steroid-pyridine derivative increased left ventricular pressure in a dose-dependent manner (0.001-100 nM); however, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These results indicate that positive inotropic activity produced by the steroid-pyridine derivative was via calcium channel activation. Furthermore, the biological activity exerted by the steroid-pyridine derivative on the left ventricle produces changes in cAMP concentration. CONCLUSION: It is noteworthy that positive inotropic activity produced by this steroid-pyridine derivative involves a different molecular mechanism compared to other positive inotropic drugs. Therefore, this steroid could be a good candidate for the treatment of heart failure.

Anti-inflammatory & anti-allergy agents in medicinal chemistry published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Computed Properties of 21829-25-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yang, Shaomei published the artcileDetermination of betahistine mesylate in tablets by ion chromatography, Formula: C10H20N2O6S2, the publication is Huagong Jishu Yu Kaifa (2011), 40(4), 27-29, database is CAplus.

The sulfur in the mol. structure of betahistine mesylate sample was converted into its oxides via combustion and further absorption by an absorbing solution to become sulfate. The sulfate in the solution was determined by ion chromatog. The amount of betahistine mesylate was derived from its stoichiometric relationship with sulfur. The calibration curve of sulfur was linear in the concentration range of 0.02-60 μg/mL. The average recovery was 98.8% with RSD of 0.15%. The method was simple, accurate and reproducible, and it could be used for the quality control of betahistine mesylate tablets.

Huagong Jishu Yu Kaifa published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C7H12ClNO, Formula: C10H20N2O6S2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Morin, Marie S. T. published the artcileCopper-Catalyzed Petasis-Type Reaction: A General Route to α-Substituted Amides From Imines, Acid Chlorides, and Organoboron Reagents, Quality Control of 971-66-4, the publication is Journal of Organic Chemistry (2012), 77(4), 2013-2017, database is CAplus and MEDLINE.

A copper-catalyzed Petasis-type reaction of imines, acid chlorides, and organoboranes to form α-substituted amides is described. This reaction does not require the use of activated imines or the transfer of special units from the organoboranes and represent a useful generalization of the Petasis reaction.

Journal of Organic Chemistry published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Quality Control of 971-66-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Figueiredo, Joana published the artcileHazard of novel anti-fouling nanomaterials and biocides DCOIT and silver to marine organisms, SDS of cas: 971-66-4, the publication is Environmental Science: Nano (2020), 7(6), 1670-1680, database is CAplus.

Biocide-based coatings have been applied for several years to tackle marine biofouling. Recently, engineered nanomaterials, such as silica mesoporous nanocapsules (SiNCs), were used to encapsulate DCOIT, an anti-fouling booster biocide, and Ag, a broad-spectrum bactericidal agent, in order to control their release with time. This study aims to assess the environmental hazard of three novel anti-fouling nanomaterials (SiNC-DCOIT, SiNC-Ag and SiNC-DCOIT-Ag) and their free counterparts (DCOIT, Ag and SiNCs) to marine ecosystems. In order to accomplish this goal, marine toxicity data (L/E/IC₅₀ or NOEC) were compiled to derive PNEC values for each compound based on statistical and deterministic approaches. The first approach relies on the hazardous concentration for 5% of the species (HC₅ using species sensitivity distribution curves) and the second relies on the lowest L/E/IC₅₀ or NOEC value, considering the appropriate assessment factors. In both approaches, PNEC values were lower for the encapsulated biocides than for their free forms. Thus, biocide encapsulation appears to be a promising solution to develop a new generation of efficient anti-fouling additives for maritime coatings with lower environmental hazard than the current state-of-the-art biocides.

Environmental Science: Nano published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, SDS of cas: 971-66-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem