Day: December 6, 2022

Trecourt, Francois published the artcileSynthesis of diazaxanthones: 5H-pyrano[2,3b:6,5-b’]dipyridin-5-one and 5H-thiopyrano[2,3-b:6,5-b’]dipyridin-5-one, Computed Properties of 71255-09-9, the main research area is pyranodipyridinone; thiopyranodipyridinone; formylation bromopyridine; pyridinecarboxaldehyde conformation.

The title compds (I; X = O, S, resp.) were prepared in 5 and 6 steps, resp., from 3-bromo-2-chloropyridine; yields were excellent. The CO bridge of the diazaxanthones was formed by coupling the aldehydes II (X = O) with 3-lithio-2-methoxypyridine and II (X = S) with 3-lithio-2-(methylthio)pyridine followed by oxidation of the resulting benzylic alc. The other bridge was formed by coupling the 2 ether or sulfide functions with pyridinium-HCl at ∼220°. The conformations of II (X = O, S) are discussed. II (X = O, S) were prepared by treatment of the 3-bromo analogs with BuLi and HCO2Et. I are the 1st reported xanthone-like heterocycles with 2 pyridine rings condensed to the 4-pyrone or -thiopyrone ring.

Journal of Chemical Research, Synopses published new progress about Cyclization. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Guoping published the artcilePost-chromatographic dicationic ionic liquid-based charge complexation for highly sensitive analysis of anionic compounds by ultra-high-performance supercritical fluid chromatography coupled with electrospray ionization mass spectrometry, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, the main research area is anion analysis UHP supercritical fluid chromatog electrospray ionization MS.

A green anal. strategy has been developed for the anal. of 10 perfluorinated compounds (PFCs) incorporating supramol. solvent (SUPRAS)-based extraction and ultra-high-performance supercritical fluid chromatog. (UHPSFC)-tandem mass spectrometry. The SUPRAS was prepared through self-assembly of reverse micelles by mixing heptanol, THF, and water at optimized volume ratios. An imidazolium-based germinal dicationic ionic liquid (DIL), 1,1-bis(3-methylimidazolium-1-yl) butylene difluoride ([C4(MIM)2]F2), was dissolved in the make-up solvent of UHPSFC and introduced post-column but before the electrospray ionization source. After chromatog. separation on a Torus DIOL anal. column (100 mm x 2.1 mm, 1.7μm), the PFC analytes associated with the DIL reagent through charge complexation. The formation of pos. charged complexes resulted in improved ionization efficiency and anal. sensitivity. Enhancement in signal intensity by one to two magnitudes was achieved in the pos. ionization mode compared to the neg. ionization mode without using the dicationic ion-pairing reagent. The developed protocol was applied to 32 samples of real textiles and 6 samples of real food packaging materials, which exhibited great potential for the anal. of anionic compounds

Analytical Chemistry (Washington, DC, United States) published new progress about Calibration. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Barker, John M. published the artcileThienopyridines. Part 7. Some electrophilic substitution reactions of thieno[2,3-b]- and -[3,2-b]pyridine isosteres of 4-oxygenated and 2,4-dioxygenated quinolines, Product Details of C10H9NO4S, the main research area is electrophilic substitution thienopyridine regiochem; quinolinone isostere electrophilic substitution.

Electrophilic substitution reactions were examined of the title compounds I, II [X = NMe, X1 = CO (III); X = CO, X1 = NH (IV), NMe (V)], VI, and VII. The 4-quinolone analogs I and IV, like the parent compound, were monobrominated and (diethylamino)methylated in the pyridine ring α to the CO group. However, whereas 4-quinolone and IV were nitrated in the pyridine ring by HNO3 alone, I was nitrated mainly in the thiophene ring at C-2 under these conditions. The methylated compounds III and V showed a similar regiochem. to their nonmethylated analogs, although their reactivity was lower. I and II were dinitrated by mixed HNO3-H2SO4 at the position α to the CO group in the pyridine ring and at either C-2 in the [2,3-b] isomers (I and III) or C-3 in the [3,2-b] compounds (IV and V); dibromination of I, III, and IV followed a similar pattern. Mannich reactions of VI and VII occurred in the pyridine rings, whereas bromination occurred in the thiophene and pyridine rings in VI and VII, resp.

Journal of Chemical Research, Synopses published new progress about Bromination. 99429-68-2 belongs to class pyridine-derivatives, name is Ethyl 4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylate, and the molecular formula is C10H9NO4S, Product Details of C10H9NO4S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Dongdong published the artcileCyclosporin population pharmacokinetics in pediatric refractory nephrotic syndrome based on real-world studies: effects of body weight and spirolactone administration, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is refractory nephrotic syndrome cyclosporin spirolactone body weight pharmacokinetics pediatrics; cyclosporin; pediatric refractory nephrotic syndrome; population pharmacokinetics; real-world study; spirolactone; weight.

Different models of population pharmacokinetics (PPK) of cyclosporin have been established in various populations. However, the cyclosporin PPK model in patients with pediatric refractory nephrotic syndrome (PRNS) has yet to be constructed. The present study aimed to establish the cyclosporin PPK model in PRNS, and to identify factors that may account for any variability. Chinese patients with PRNS treated with cyclosporin between June 2014 and June 2018 at the Children’s Hospital of Fudan University (Shanghai, China) were retrospectively analyzed. The impact of demog. features, laboratory parameters and concomitant medications was evaluated. A total of 18 PRNS patients from real-world studies were analyzed by non-linear mixed-effects modeling. A one-compartment model with first-order absorption and elimination was selected as the appropriate model in PRNS. Body weight (WT) and spirolactone intake were included as significant covariates for the apparent oral clearance (CL/F), and the WT was revealed to significantly influence the apparent volume of distribution (V/F). The final covariate models were as follows: CL/F = 80.7 × (WT/70)0.75 × (1-0.265 × θspirolactone), and V/F = 2,030 × (WT/70), where θspirolactoneis the coefficient of spirolactone. The inter-individual variability in CL/F and V/F was 44.6 and 53.1%, resp. In conclusion, in the present study, a cyclosporin PPK model for patients with PRNS was successfully constructed, and the presence of a clin. significant interaction between spirolactone and cyclosporin in PRNS patients was determined based on real-world studies, indicating that concomitant medication with spirolactone was able to reduce cyclosporin clearance in the patients with PRNS.

Experimental and Therapeutic Medicine published new progress about Body weight. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lee, Stephanie M. published the artcileL-type calcium channels contribute to ethanol-induced aberrant tangential migration of primordial cortical GABAergic interneurons in the embryonic medial prefrontal cortex, COA of Formula: C17H18N2O6, the main research area is LTCC embryonic mPFC ethanol primordial cortical GIN tangential migration; FASD; GABA; alcohol; calcium; calcium channels; interneuron.

Exposure of the fetus to alc. (ethanol) via maternal consumption during pregnancy can result in fetal alc. spectrum disorders (FASD), hallmarked by long-term phys., behavioral, and intellectual abnormalities. In our preclin. mouse model of FASD, prenatal ethanol exposure disrupts tangential migration of corticopetal GABAergic interneurons (GINs) in the embryonic medial prefrontal cortex (mPFC). We postulated that ethanol perturbed the normal pattern of tangential migration via enhancing GABAA receptor-mediated membrane depolarization that prevails during embryonic development in GABAergic cortical interneurons. However, beyond this, our understanding of the underlying mechanisms is incomplete. Here, we tested the hypothesis that the ethanol-enhanced depolarization triggers downstream an increase in high-voltage-activated nifedipine-sensitive L-type calcium channel (LTCC) activity and provide evidence implicating calcium dynamics in the signaling scheme underlying the migration of embryonic GINs and its aberrance. Tangentially migrating Nkx2.1+ GINs expressed immunoreactivity to Cav1.2, the canonical neuronal isoform of the L-type calcium channel. Prenatal ethanol exposure did not alter its protein expression profile in the embryonic mPFC. However, exposing ethanol concomitantly with the LTCC blocker nifedipine prevented the ethanol-induced aberrant migration both in vitro and in vivo. In addition, whole-cell patch clamp recording of LTCCs in GINs migrating in embryonic mPFC slices revealed that acutely applied ethanol potentiated LTCC activity in migrating GINs. Based on evidence reported in the present study, we conclude that calcium is an important intracellular intermediary downstream of GABAA receptor-mediated depolarization in the mechanistic scheme of an ethanol-induced aberrant tangential migration of embryonic GABAergic cortical interneurons.

eNeuro published new progress about Body weight. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, COA of Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dzodic, Predrag published the artcileA reliable chromatographic method for the simultaneous determination of ciprofloxacin and moxifloxacin in human serum, Synthetic Route of 72509-76-3, the main research area is serum ciprofloxacin moxifloxacin high performance liquid chromatog.

Purpose: To develop and validate a simple chromatog. method for the anal. of ciprofloxacin and moxifloxacin in human serum. Methods: After protein precipitation had been performed, high performance liquid chromatog. (HPLC) with UV detection was utilized for the anal. of ciprofloxacin and moxifloxacin in human serum. Anal. column Zorbax SB-C18 (150 mm x 4.6 mm i.d., particle size 3.5μm) was used as a stationary phase. Chromatog. separation was realized with the mobile phase 0.1% trifluoroacetic acid in water for chromatog. – methanol (66:34, volume/volume), at the flow rate of 1 mL/min, temperature of 35°C and detection at 280 nm. The method validation was performed according to the guidelines of the European Medicines Agency (EMA). Results: The chromatog. run time was about 12 min and no interference was observed For ciprofloxacin, the method was linear over a concentration range of 0.5-50μg/mL, with a correlation coefficient of 0.9874. For moxifloxacin, the method was linear over a concentration range of 0.5-50μg/mL, with a correlation coefficient of 0.9946. Since relative standard deviation (RSD) and relative recovery values were within acceptable limits according to EMA guidelines, good intra-day precision, inter-day precision, as well as the accuracy of the method, were observed Conclusion: A simple and reliable HPLC-UV method has been developed and validated for the simultaneous determination of ciprofloxacin and moxifloxacin in human serum. The method can be applied for therapeutic drug monitoring but also and pharmacokinetic studies of ciprofloxacin and moxifloxacin.

Tropical Journal of Pharmaceutical Research published new progress about Blood serum. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yu, Qiuli published the artcileEffects of drinking water fluorosis on L-type calcium channel of hippocampal neurons in mice, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is drinking water fluorosis calcium channel hippocampal neuron; Calcium imbalance; Fluorosis; Hippocampal CA1 region; LTCCs; Patch clamp.

The study aimed to investigate the effects of drinking water fluorosis on L-type calcium channels (LTCCs) in mouse hippocampal neurons. A total of 60 newly weaned ICR male mice were randomly divided into control, low fluoride and high fluoride groups. After 3 and 6 mo of exposure to fluoride, the patch clamp technique was used to detect the peak and relative values (I/Imax), steady-state activation curve ratio (G/Gmax), decay time constant, and tail current time constant of LTCCs currents in hippocampal CA1 region of mouse brain slices. Fluoride greatly reduced the serum and urinary calcium concentrations in mice, and the chronic fluorosis has a greater impact than subchronic fluorosis. The peak value of LTCCs current in pyramidal neurons of hippocampal CA1 area was significant and increased with the prolonged exposure time. The relative values of current and steady-state coefficients were changed greatly. The decay and tail current time increased significantly. High fluorine concentration indicates great peak value and open time of LTCCs opening. LTCCs are sensitive to fluoride exposure. The activation voltage of calcium channels induced by fluoride exposure is decreased, the opening time of calcium channels is prolonged, and the calcium influx per unit time increased, thereby overloading calcium concentration in neurons and this may be an explanation for intracellular calcium overload caused by fluoride. The imbalance of calcium metabolism caused by fluorosis may be a pathogenesis of brain injury induced by fluoride. Furthermore, the risk of brain damage from low-fluorine exposure cannot be ignored.

Chemosphere published new progress about Blood serum. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sehdev, Bhumika published the artcileEffect of calcium channel blockers on gingival tissues in hypertensive patients visiting Ayder Referral Hospital, Mekelle, Ethiopia, Category: pyridine-derivatives, the main research area is hypertensive patients gingival tissue calcium channel blocker.

Long term treatment of common chronic cardiac conditions such as hypertension with Calcium channel blockers (CCBs) has been associated with gingival hyperplasia. This oral side effect may affect esthetics and function, yet often overlooked and therefore underreported among hypertensive patients visiting in Ayder Comprehensive Specialized Hospital, Mekelle, Ethiopia. This study aims to determine the association of CCBs with gingival overgrowth in hypertensive patients. This is hospital based cross sectional study conducted among 50 hypertensive patients (25 CCBs and 25 non-CCBs age matched controls) attending the medical outpatient clinic of Ayder Comprehensive Specialized hospital. Data collection tools included interviewer administered questionnaires and periodontal examination Socio-demog. details, medical history and periodontal indexes (plaque index, papillary bleeding index, grade of GO according to DIGO clin. index) were recorded. The mean plaque index and mean papillary bleeding index for CCB users were 0.9±0.8 and 0.3±0.5 resp., while mean plaque index and mean papillary bleeding index for non-CCB users were 1.4±0.8 and 0.8±1.3 mm resp. Also, more females (44%) presented with DIGO compared to males (26%) in both the groups. Participants on CCBs had significantly increased probing depths than that of the non-CCB users (p = 0.001). The higher prevalence of DIGO among CCB users compared with non-CCB users has been reported. Furthermore, there was an increased risk of GO nearly 3 folds in CCB users compared with non-CCB users. The slightly higher finding of DIGO among Nifedipine users in the current study may be related to the fact that more patients were placed on Nifedipine. The significant association between increased probing depth and DIGO in our study was not unexpected owing to the formation of false pocketing in relation to GO. The study reveals that the risk of GO is nearly three times higher in CCB than non-CCB users and 2 folds in nifedipine than amlodipine users in Mekelle. Further studies intend to conduct multicenter studies with larger sample sizes to further elucidate the effect of the dose and duration of CCB on DIGO and also consider genetic studies for DIGO among Mekelle patients on CCB.

International Journal of Pharmaceutical, Chemical and Biological Sciences published new progress about Anesthetics. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Buchwald, Peter published the artcileSoft drugs: design principles, success stories, and future perspectives, Quality Control of 72509-76-3, the main research area is Soft drug design success story future perspective; Antedrug; drug metabolism; esterases; methylphenidate; prodrug; sofpironium; therapeutic index; toxic metabolite.

In the present study, the SD concept is part of the more general recognition that drug design needs to fully integrate metabolic con-siderations from the very beginning as metabolites contribute significantly to the overall activity and toxicity profile of the original drug and focus not on improving activity alone, but on improving the activity/toxicity ratio. This is usually characterized by the therapeutic index, typically defined as the ratio between the half-maximal toxic and effec-tive doses: TI = TD50/ED50. These ideas are the main underlying principles of retrometabolic drug design, which incorporates both SD and chem. delivery system (CDS) design. For most drugs, several metabolites are formed following administration, and they can contribute significantly not just to the overall activity, but also to toxicity and side effects. This can lead to complex time-profiles as illustrated in Figure 1(a), which shows the case of a hypothetical drug D that is present together with its active, toxic, and inactive metabolites. In light of these, the SD approach, which provides general drug design strategies, has particular potential. Because it often starts from a known active structure and focuses on designing safer drugs by decreasing side effects and toxicity, the likelihood of success is increased, especially considering the perspective highlighted by Sir James Black: the most fruitful basis for the discovery of a new drug is to start with an old drug.

Expert Opinion on Drug Metabolism & Toxicology published new progress about Anesthetics. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Quality Control of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Young, Summer E. published the artcileSynthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets, SDS of cas: 321438-86-2, the main research area is proteinase activated receptor PAR4.

Protease activated receptor-4 [PAR4, proteinase-activated receptor PAR-4] is one of thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. The authors sought to develop potent, selective and novel PAR4 antagonists to test the role of PAR4 in thrombosis and hemostasis. The development of an expedient three-step synthetic route to access a novel series of indole-based PAR4 antagonists also necessitated the development of a platelet based high-throughput screening assay. Screening and subsequent structure activity relationship anal. yielded several selective PAR4 antagonists as well as possible new scaffolds for future antagonist development. The title compounds thus formed included an indole benzoic acid ester (I) and related substances. I was evaluated against an indazole benzoic acid ester analog (II) [i.e., 4-[1-(phenylmethyl)-1H-indazol-3-yl]benzoic acid Et ester]. The synthesis of the target compounds was achieved using 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole as starting materials. The synthetic sequence involved an alkylation of 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole, formation of bromide derivatives and a subsequent coupling reaction with boronic acids.

PLoS One published new progress about Allosterism. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, SDS of cas: 321438-86-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem