Pyridine-derivatives

Oikonomou, Katerina D. published the artcileCalcium dysregulation and compensation in cortical pyramidal neurons of the R6/2 mouse model of Huntington′s disease, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Huntington disease calcium dysregulation cortical pyramidal neuron; Huntington’s disease; R6/2 mice; calcium imaging; cortical pyramidal neurons; dantrolene; two-photon laser scanning microscopy.

Huntington′s disease (HD) is a fatal, hereditary neurodegenerative disorder that predominantly affects striatal medium-sized spiny neurons and cortical pyramidal neurons (CPNs). It has been proposed that perturbations in Ca2+ homeostasis could play a role in CPN alterations. To test this hypothesis, we used the R6/2 mouse model of juvenile HD at different stages of disease progression; presymptomatic, early symptomatic, and late symptomatic. We combined whole-cell patch-clamp recordings of layer 2/3 CPNs with two-photon laser scanning microscopy to image somatic and dendritic Ca2+ transients associated with evoked action potentials (APs). We found that the amplitude of AP-induced Ca2+ transients recorded at the somata of CPNs was significantly reduced in presymptomatic and late symptomatic R6/2 mice compared with wild-type (WT) littermates. However, reduced amplitudes were compensated by increases in decay times, so that Ca2+ transient areas were similar between genotypes. AP-induced Ca2+ transients in CPN proximal dendrites were variable and differences did not reach statistical significance, except for reduced areas in the late symptomatic group. In late symptomatic mice, a specific store-operated Ca2+ channel antagonist, EVP4593, reduced somatic Ca2+ transient amplitude similarly in WT and R6/2 CPNs. In contrast, dantrolene, a ryanodine receptor (RyR) antagonist, and nifedipine, an L-type Ca2+ channel blocker, significantly reduced both somatic Ca2+ transient amplitude and area in R6/2 but not WT CPNs. These findings demonstrate that perturbations of Ca2+ homeostasis and compensation occur in CPNs before and after the onset of overt symptoms, and suggest RyRs and L-type Ca2+ channels as potential targets for therapeutic intervention. NEW & NOTEWORTHY We used two-photon microscopy to examine calcium influx induced by action potentials in cortical pyramidal neurons from a mouse model of Huntington′s disease (HD), the R6/2. The amplitude of somatic calcium transients was reduced in R6/2 mice compared with controls. This reduction was compensated by increased decay times, which could lead to reduced calcium buffering capacity. L-type calcium channel and ryanodine receptor blockers reduced calcium transient area in HD neurons, suggesting new therapeutic avenues.

Journal of Neurophysiology published new progress about Animal cell, somatic. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Franze, Silvia published the artcileDrug-in-micelles-in-liposomes (DiMiL) systems as a novel approach to prevent drug leakage from deformable liposomes, COA of Formula: C17H18N2O6, the main research area is micelles liposome drug delivery systems; Elastic vesicles; Ethosomes; Nifedipine; Piroxicam; Transdermal; Transethosomes; Transfersomes.

Deformable liposomes (DL) are successfully exploited to enhance the skin penetration of several compounds Nevertheless, the “”soft”” nature of the bilayer favors the drug leakage, mainly in the case of hydrophobic compounds This work aimed to develop a suitable strategy to stabilize the lipid bilayer, without compromising the deformability properties of DL. The approach relied on the design of a “”matryoshka”” system, namely a drug in micelles in deformable liposomes (DiMiL) system. The performances (drug leakage, deformability and in vitro skin penetration profile) of DiMiLs were tested using nifedipine and piroxicam as model compounds and compared to those of traditional DL. The micelles were made of Kolliphor HS15 whereas the lipid vesicles were composed of egg-phosphatidylcholine and Tween 80 (T80) at 95:5 or 85:15 weight/weight ratios. As expected, the drug leakage from DL was high after only one month of storage (almost 50% in the case of nifedipine and in the range of 39-79% in the case of piroxicam loaded DL, depending on T80 content). Optimized DiMiL formulations retained instead the drug content up to two-months storage period. Moreover, the constant of deformability of DiMiLs felt in the acceptance range for deformable vesicles intended for cutaneous application and the skin permeated amount of the delivered drugs was increased of at least 4 times. In conclusion, DiMiL reveals to be a suitable approach to avoid the leakage of hydrophobic compounds and an attractive transdermal drug delivery system for poorly permeable drugs.

European Journal of Pharmaceutical Sciences published new progress about Drug delivery systems. 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

Claude-Montigny, B. published the artcileMicroenvironment effects on the kinetics of electron-transfer reactions involving dithionite ions and viologens. 2. Stabilization of ion radicals by polyelectrolytes and dimerization kinetics of dialkyl viologens, Synthetic Route of 36437-30-6, the main research area is viologen cation radical dimerization polyelectrolyte stabilizer.

The dimerization kinetics of reduced dialkyl viologens (di-C4, di-C7, and di-C8 cation radicals) was studied in the presence of polyelectrolytes poly(styrenesulfonate) (PSSH) or the polysoap MA-CVE (maleic acid/cetyl vinyl ether copolymer). Three kinetic models were considered: total dimerization (I), reversible dimerization (II) with initial concentration of reduced viologen equal to the stoichiometric concentration, and (III) reversible dimerization with finite dimer at time 0. In the absence of polyelectrolyte, the quality of fit to the exptl. kinetics was independent of model I-III; the rate of dimerization increased from di-C7 to di-C8, consistent with decreasing solubility and increasing degree of association in this series. The disappearance of reduced viologen is suppressed by polyelectrolyte; here, too, models I-III did not drastically differ.

Journal of Physical Chemistry published new progress about Dimerization kinetics. 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, Synthetic Route of 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yilmaz, Osman published the artcileEffects of nifedipine on fetal cardiac function in preterm labor, Formula: C17H18N2O6, the main research area is mitral valve fetus preterm labor nifedipine; fetal cardiac functions; myocardial performance index; nifedipine; preterm labor; sphericity index.

To evaluate the effects of nifedipine treatment on fetal hemodynamics and cardiac function during preterm labor. This prospective study assessed several quant. parameters of fetal cardiac circulation and function, and found no significant changes at 48 h after nifedipine treatment. These findings suggest that tocolytic nifedipine may be safe for fetuses. It supports clinicians to use nifedipine treatment for tocolysis without any cardiac effect on the fetus. A prospective cohort study was conducted at a tertiary hospital between Jan. 2016 and Oct. 2017. A total of 45 pregnant women who required nifedipine for preterm labor were included in this study. Fetal Doppler ultrasound was performed and fetal systolic and diastolic function was measured prior to, and 48 h after, the first nifedipine treatment. Conventional Doppler parameters were used to evaluate fetal heart function and hemodynamic changes. Tricuspid annular plane systolic excursion, mitral annular plane systolic excursion and the sphericity index were also evaluated to assess changes in fetal cardiac morphol. No significant changes in fetal Doppler parameters were observed following nifedipine tocolysis. There was no significant difference in the fetal cardiac function parameters of both ventricles before vs. after nifedipine treatment. Tricuspid annular plane systolic excursion, mitral annular plane systolic excursion, and sphericity index values were unchanged following nifedipine treatment.

Journal of Perinatal Medicine published new progress about Cardiovascular system. 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, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Jinggui published the artcileEfficacy and safety of combination of magnesium sulfate, phentolamine and nifedipine in treatment of patients with hypertensive disorder complicating pregnancy, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is magnesium sulfate phentolamine nifedipine hypertensive disorder pregnancy; hemodynamics; hypertensive disorder complicating pregnancy; magnesium sulfate; nifedipine; phentolamine; urinary protein.

Efficacy and safety of the combination of magnesium sulfate, phentolamine and nifedipine in the treatment of patients with hypertensive disorder complicating pregnancy (HDCP) and its effect on hemodynamics and urinary protein level were investigated. One hundred and six patients with HDCP diagnosed at the Affiliated Hospital of Beihua University from Feb. 5, 2016 to May 9, 2017 were retrospectively analyzed. Patients were divided into the magnesium sulfate group and the combination group, according to the therapeutic schemes. The efficacy 1 wk later was observed The general clin. data of the patients were recorded, and data were acquired with respect to hemodynamic indexes before and after treatment [changes of S/D ratio of umbilical artery flow, and cardiac index and total peripheral resistance (TPR)], the 24-h urinary protein level, clin. efficacy and safety [adverse drug reactions (ADR) and maternal and neonatal outcomes]. Before treatment, there was no statistically significant difference between the two groups in terms of S/D ratio of umbilical artery flow (P>0.05), while after treatment the S/D ratio was significantly lower than that before treatment in both groups (P<0.05). Before treatment, there was no statistically significant difference between the two groups in terms of cardiac index (P>0.05). TPR after treatment was significantly lower than that before treatment in both groups (P<0.001). Compared with the magnesium sulfate group, patients in the combination group had significantly lower 24-h urinary protein level after treatment (P<0.001), significantly higher total effective rate (P<0.05), significantly lower incidence rate of ADR (P<0.001), and significantly lower incidence rate of adverse maternal and neonatal outcomes (P<0.001). In conclusion, the combination of magnesium sulfate, phentolamine and nifedipine can significantly improve the hemodynamic indexes, the 24-h urinary protein level, the clin. efficacy, ADR and maternal and neonatal outcomes of patients with HDCP, therefore it is worthy of use in the clinic. Experimental and Therapeutic Medicine published new progress about Cardiovascular system. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Giri, T. published the artcileSynthesis and antibacterial activity of novel 4-{4-(methylamino)thieno[3,2-d]pyrimidin-2-yl}-benzohydrazide derivatives, Computed Properties of 71255-09-9, the main research area is methylaminothienopyrimidinyl benzohydrazide derivative preparation antibacterial agent.

A series of novel 4-{4-(methylamino)thieno[3,2-d]pyrimidin-2-yl}benzohydrazide derivatives were synthesized and evaluated for their antibacterial activity. Most of the compounds demonstrated high activity towards Escherichia coli, Pseudomonas, Staphylococcus aureus, and Bacillus. Structures of all synthesized compounds were confirmed by spectral anal.

Russian Journal of General Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Mitsui, Retsu published the artcileRole of K+ channels in maintaining the synchrony of spontaneous Ca2+ transients in the mural cells of rat rectal submucosal arterioles, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is potassium channel calcium mural cell rectal precapillary arteriole; Intercellular synchrony; K+ channels; Microvasculature; Mural cells; Spontaneous Ca2+ transient.

Mural cells in precapillary arterioles (PCAs) generate spontaneous Ca2+ transients primarily arising from the periodic release of Ca2+ from sarcoendoplasmic reticulum (SR/ER). The Ca2+ release induces Ca2+-activated chloride channel (CaCC)-dependent depolarisations that spread to neighboring mural cells to develop the synchrony of their Ca2+ transients. Here, we explored the roles of K+ channels in maintaining the synchrony of spontaneous Ca2+ transients. Intracellular Ca2+ dynamics in mural cells were visualised by Cal-520 fluorescence Ca2+ imaging in the submucosal PCAs of rat rectum. Increasing extracellular K+ concentration ([K+]o) from 5.9 to 29.7 mM converted synchronous spontaneous Ca2+ transients into asynchronous, high-frequency Ca2+ transients. Similarly, the blockade of inward rectifier K+ (Kir) channels with Ba2+ (50μM) or Kv7 voltage-dependent K+ (Kv7) channels with XE 991 (10μM) disrupted the synchrony of spontaneous Ca2+ transients, while the blockers for large-, intermediate- or small-conductance Ca2+-activated K+ channels had no effect. Kir2.1 immunoreactivity was detected in the arteriolar endothelium but not mural cells. In the PCAs that had been pretreated with XE 991 or Ba2+, nifedipine (1μM) attenuated the asynchronous Ca2+ transients but failed to restore their synchrony. In contrast, levcromakalim, an ATP-sensitive K+ channel opener, restored the synchronous Ca2+ transients. Thus, constitutively active Kv7 and Kir channels appear to be involved in maintaining the relatively hyperpolarised membrane of mural cells. The hyperpolarised membrane prevents depolarisation-induced ‘premature’ Ca2+ transients to ensure sufficient SR/ER Ca2+ refilling that is required for regenerative Ca2+ release resulting in synchronous Ca2+ transients amongst the mural cells.

Pfluegers Archiv published new progress about Arterial endothelium, arteriolar endothelium (precapillary). 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

Amino, Yusuke published the artcileNovel method for the synthesis of 2′,3′-unsaturated nucleosides from 2′(3′)-acetoxy-3′(2′)-halogeno derivatives by using sodium dithionite with viologen as a reductive elimination mediator, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, the main research area is viologen mediated reductive elimination acetylbromodeoxy nucleoside; unsaturated dideoxy nucleoside.

Reductive elimination of vicinal acetylated halohydrins with Na2S2O4 as the reducing agent and viologen as the reduction mediator in a 2-phase water-organic system is described. 2′,3′-Unsaturated nucleosides such as 1-(5-O-acetyl-2,3-dideoxy-β-D-glycero-pent-2-enofuranosyl)adenine (I), -hypoxanthine, and -uracil were obtained from 2′(3′)-acetoxy-3′(2′)-halogeno derivatives, e.g., II, in good yields by means of this procedure.

Chemical & Pharmaceutical Bulletin published new progress about Nucleosides Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Zhang, Youcan published the artcileCopper-catalyzed carbonylative synthesis of pyrrolidine-containing amides from γ,δ-unsaturated aromatic oxime esters, Related Products of pyridine-derivatives, the main research area is pyrrolidine containing amide preparation regioselective copper catalyst; unsaturated aromatic oxime ester amine carbonylative cyclization.

A new method of low-cost copper-catalyzed carbonylative cyclization for preparing pyrrolidine-containing amides I (R = H, R’ = t-Bu, Ph, 2-Py, etc; R1 = Me, Et, Ph, R2 =Me, Allyl, CHC6H5; Ar = Ph, 3-MeC6H4, 2-thiophenenyl, 2-Naph, etc.; R3, R4 = H, Me;) from γ,δ-unsaturated aromatic oxime esters II and amines has been described. A range of readily available amines were examined, including primary, secondary, and heterocycle amines, giving over 60 examples of targeted N-heterocycle substituted amides with broad functional group tolerance, good chem. selectivity and moderate to excellent yields.

Organic Chemistry Frontiers published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Ling published the artcileMechanochemical enzymatic synthesis of 1,4-dihydropyridine calcium antagonists and derivatives, Application In Synthesis of 72509-76-3, the main research area is Lipozyme ball milling dihydropyridine calcium antagonists.

BACKGROUND : Enzyme promiscuity has attracted significant attention from chemists and biochemists in recent years. However, long reaction time and use of toxic organic solvents limit its applications for industrial processes. 1,4-Dihydropyridine (1,4-DHP) calcium antagonists are recommended for the first line treatment of hypertension. Although some chem. protocols for the preparation of 1,4-DHP calcium antagonists have been developed, enzymic synthesis of these compounds still remains uncovered. RESULTS : Solvent-free quick synthesis of 1,4-DHP calcium antagonists felodipine, nitrendipine, nifedipine and nemadipine B and their derivatives was achieved by Lipozyme RM IM (triacylglycerol acylhydrolase, EC3.1.1.3)-catalyzed multicomponent reactions of aromatic aldehyde, alkyl acetoacetate and alkyl 3-aminocrotonate under ball-milling conditions. The products were obtained in moderate yields (up to 86.8%) and the influence of reaction conditions including catalyst loading, grinding auxiliary and grinding frequency was investigated. CONCLUSION : The protocol successfully overcame some longstanding problems in the field of enzymic promiscuity research, such as long reaction time and use of harmful organic solvents, and demonstrated the potential application value of promiscuous enzyme-catalyzed reactions under ball-milling conditions for pharmaceutical synthesis. © 2019 Society of Chem. Industry.

Journal of Chemical Technology and Biotechnology published new progress about Pharmaceutical natural products (1,4-Dihydropyridine calcium). 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, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem