Category: pyridine-derivatives

Shankpal, Pramod published the artcileEvaluation of anti-anxiety effect of nifedipine compared to diazepam in swiss albino mice using behavioural models, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is nifedipine diazepam anxiolytic dihydropyridines elevated plus maze behavioral model.

The present study was undertaken to evaluate the acute and chronic anxiolytic effects of nifedipine in comparison to diazepam using in Swiss Albino mice using two behavioral models. 30 Swiss albino mice were divided into 5 groups with 6 mice in each group. The study was conducted in two phases to evaluate acute and chronic effects. The groups consisted of diazepam (1 mg/kg), 3 doses of nifedipine (2.6 mg/kg, 5.2 mg/kg and 10.4 mg/kg) and vehicle control. The Elevated Plus Maze (EPM) and Light and Dark box were used to evaluate the anti-anxiety effects. The number of entries and time spent in the open arm of the elevated plus-maze and in the light area of light and dark box model were noted and compared among the 5 groups. Observations were analyzed using ANOVA and post hoc Tukey’s test. Nifedipine (5.2 mg/kg and 10.4 mg/kg) significantly increased the number of entries and time spent in the open arm compared to vehicle control in the EPM test (p < 0.001). Similarly, in the light and dark box test, nifedipine (5.2 mg/kg and 10.4 mg/kg) increased the number of entries and time spent in the light area compared to vehicle control (p < 0.05). However, the low dose of nifedipine (2.6 mg/kg) did not exhibit significant findings. Two doses of nifedipine (5.2 mg/kg and 10.4 mg/kg) possess anti-anxiety effects both on acute and chronic administration in both elevated plus maze and light and dark box model. International Journal of Pharmacy and Pharmaceutical Sciences published new progress about Amygdala. 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, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Moreau, Magali published the artcileA baseline assessment of emerging organic contaminants in New Zealand groundwater, Product Details of C18H19Cl2NO4, the main research area is emerging organic contaminant baseline assessment groundwater pollution New Zealand; Emerging organic contaminant; Groundwater; Groundwater quality; Monitoring; New Zealand; Waikato region.

Emerging organic contaminants (EOC) are manufactured compounds, used for a variety of purposes, are a rising concern for freshwater quality and human and aquatic health. Their occurrence in groundwater was demonstrated in several international surveys. This work conducted the first baseline survey on EOC occurrence in New Zealand groundwater, using a wide-screening approach (723 compounds) and a novel stratified to mean residence time (MRT) randomized design to inform future monitoring. A total of 61 sites were sampled: 51 baseline sites from State of the Environment network in the Waikato region, and 10 targeted sites near known EOC sources for comparison. EOC were detected at 91% of baseline sites at concentrations of 0.1-11,000 ng/L. Multiple EOC groups were encountered: pesticides (48 compounds), pharmaceuticals (11), industrial (10), preservatives/food additives (3), and personal care products (1). Similar EOC diversity and concentration range were observed at targeted sites, with the addition of drugs of abuse and life-style compounds EOC detections occurred across young (1-11 yr. MRT), intermediate (11-50 yr. MRT), and old (50-250 yr. MRT) groundwater with higher concentrations and more types of EOC detected at sites with the youngest groundwater. Concentrations of 73 compounds detected at baseline sites were comparable to those observed in overseas groundwater, with 28 compounds measured at concentrations greater than the European Union maximum admissible concentration for pesticides. Survey results were used to: review current pesticide monitoring; propose complementary monitoring; identify potential EOC groundwater tracers; and identify compounds for which cost-effective, national laboratory capability is needed. Waikato survey results demonstrated ubiquitous occurrence of un-monitored, unregulated EOC in groundwater and limitations for using targeted approaches to establish monitoring.

Science of the Total Environment published new progress about Aquifers. 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, Product Details of C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Maiden, Tracy M. M. published the artcileSynthesis of Functionalized Pyridines via a Regioselective Oxazoline Promoted C-H Amidation Reaction, Recommanded Product: Ethyl 6-chloropicolinate, the main research area is oxazolylpyridine functionalized preparation rhodium silver catalyzed amidation; azaquinazoline scaffold preparation; pyridopyrimidinone preparation; nicotinamide derivative preparation heterocyclization; picolinamide derivative preparation heterocyclization.

The 1st Rh-catalyzed C-H amidation of pyridines is reported. The incorporation of a substituent at the C2 position both is crucial to the success of this transformation and provides considerable scope for further elaboration of the resulting products. Among these compounds, 2-chloropyridines allow access to a selection of intermediates including a versatile azaquinazoline scaffold.

Organic Letters published new progress about Amidation. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, Recommanded Product: Ethyl 6-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Young, Ian S. published the artcilePalladium-Catalyzed Site-Selective Amidation of Dichloroazines, Synthetic Route of 132097-09-7, the main research area is dichloroazine amide amidation palladium; chloroazinyl amide regioselective preparation; palladium amidation catalyst.

A highly site-selective amidation reaction of substituted 2,4-dichloroazines is reported. Palladium acetate/1,1′-bis(diphenylphosphino)ferrocene (dppf) was identified as the optimal catalyst system, producing >99:1 C-2/C-4 selectivity for most examples. The generality of this transformation was demonstrated through a survey of a diverse amide/substituted 2,4-dichloroazine scope, leading to the preparation of the desired C-2 amidated products in good to excellent yields.

Organic Letters published new progress about Amidation. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Synthetic Route of 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

den Hertog, H. J. published the artcileHetarynes. VI. Amination of bromoethoxypyridines, SDS of cas: 17117-13-4, the main research area is .

cf. CA 58, 11325a; 60, 1724d. Some bromoethoxypyridines were aminated with KNH2 in liquid NH3. The 3-bromo- and 4-bromoethoxypyridines reacted via hetaryne intermediates. The reaction of 2-bromo-6-ethoxypyridine proceeded via a rearrangement. 2-Bromo-4-ethoxypyridine, b2 104-6°, m. 35-6°, was prepared by treating 2-bromo-4-hydroxypyridine with diazoethane in Et2O for 16 hrs. at room temperature 4-Bromo-2-ethoxypyridine, m. 5.5-7°, was prepared from 4-amino-2-ethoxypyridine. Amination was carried out by adding 2.5 millimoles of the bromoethoxypyridine in Et2O to a solution prepared from 10 millimoles K and 30-40 ml. liquid NH3 in the presence of Fe(NO3)3 at -33° over a period of 10 min. (with stirring). The reaction-was stopped with 12 millimoles NH4Cl and the mixture evaporated, extracted with Et2O, and analyzed by gas chromatography. The following results were obtained [bromoethoxypyridine used and the aminoethoxypyridine(s) (molar ratio) produced given]: 4-bromo-2-ethoxy, 3-amino-2-ethoxy[-(1-2%)], 4-amino-2-ethoxy[-(98-99%)]; 4-bromo-3-ethoxy, 5-amino-3-ethoxy; 3-bromo-2-ethoxy, 3-amino-2-ethoxy (3), 4-amino-2-ethoxy (97); 3-bromo-4-ethoxy, 2-amino-4-ethoxy (55-60), 2-amino-5-bromo-4-ethoxy (15-20), 4-ethoxy (25); 3-bromo-5-ethoxy, 3-amino-5-ethoxy; 3-bromo-6-ethoxy, 3-amino-6-ethoxy (35), 4-amino-6-ethoxy (65); 2-bromo-3-ethoxy, 2-amino-3-ethoxy (99), 3-ethoxy (1); 2-bromo-4-ethoxy, 2-amino-4-ethoxy; 2-bromo-5-ethoxy, 2-amino-5-ethoxy (90-95), 5-ethoxy (5-10); 2-bromo-6-ethoxy, 2-amino-6-ethoxy (80-85), 4-amino-6-ethoxy (10-15).

Recueil des Travaux Chimiques des Pays-Bas published new progress about Amination. 17117-13-4 belongs to class pyridine-derivatives, name is 2-Bromo-4-ethoxypyridine, and the molecular formula is C7H8BrNO, SDS of cas: 17117-13-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Segura-Chama, Pedro published the artcileModulation of intracellular calcium concentration by D2-like DA receptor agonists in non-peptidergic DRG neurons is mediated mainly by D4 receptor activation, Quality Control of 21829-25-4, the main research area is calcium DA receptor DRG neuron D4receptor; Ca(2+) microfluorometry; Ca(V)2.2 Ca(2+) channels; D2-like receptors; D4 receptor; Depolarization-elicited [Ca(2+)](i) increase; Small non-peptidergic DRG neurons.

Nociceptive stimuli attributes are codified in the periphery; at this level, D2-like dopamine (DA) receptor activation decreases the high voltage-gated Ca2+ current predominantly in mechanonociceptive neurons, which explains the presynaptic action mechanism of the antinociception produced by quinpirole when it is intrathecally administered in rats. However, the identity of D2-like DA receptor subtype that mediates this effect remains unknown. To answer this question, we used Fluo-4-based Ca2+ microfluorometry to study the depolarization-elicited [Ca2+]i increase in small non-peptidergic DRG neurons (identified by its binding to the Isolectin B4), and to test the effect of D2-like DA receptor activation by quinpirole in presence of selective antagonists for D2, D3, and D4 DA receptors. The results showed a significantly greater contribution of the D4 DA receptor in the down-modulation of depolarization-elicited [Ca2+]i increase in small non-peptidergic DRG neurons compared to the other receptors. Although the D2 and D3 receptor antagonists also slightly inhibited the effect of quinpirole, their effects were significantly weaker than those of the D4 receptor antagonist. Furthermore, we showed that quinpirole selectively inhibits the CaV2.2 Ca2+ channels. Our results suggest that the activation of the D4 DA receptors is a promising strategy for pain management at the spinal cord level.

Neuroscience Letters published new progress about Analgesia. 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, Quality Control of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chovancova, Barbora published the artcileCalcium signaling affects migration and proliferation differently in individual cancer cells due to nifedipine treatment, Computed Properties of 21829-25-4, the main research area is calcium signaling cancer migration proliferation nifedipine; Apoptosis; Breast cancer; Inositol 1,4,5-trisphosphate receptor; Migration; Sodium calcium exchanger 1.

Several papers have reported that calcium channel blocking drugs were associated with increased breast cancer risk and worsened prognosis. One of the most common signs of breast tumors is the presence of small deposits of calcium, known as microcalcifications. Therefore, we studied the effect of dihydropyridine nifedipine on selected calcium transport systems in MDA-MB-231 cells, originating from triple neg. breast tumor and JIMT1 cells that represent a model of HER2-pos. breast cancer, which possesses amplification of HER2 receptor, but cells do not response to HER2 inhibition treatment with trastuzumab. Also, we compared the effect of nifedipine on colorectal DLD1 and ovarian A2780 cancer cells. Both, inositol 1,4,5-trisphosphate receptor type 1 (IP3R1) and type 1 sodium calcium exchanger (NCX1) were upregulated due to nifedipine in DLD1 and A2780 cells, but not in breast cancer MDA-MB-231 and JIMT1 cells. On contrary to MDA-MB-231 and JIMT1 cells, in DLD1 and A2780 cells nifedipine induced apoptosis in a concentration-dependent manner. After NCX1 silencing and subsequent treatment with nifedipine, proliferation was decreased in MDA-MB-231, increased in DLD1 cells, and not changed in JIMT1 cells. Silencing of IP3R1 revealed increase in proliferation in DLD1 and JIMT1 cells, but caused decrease in proliferation in MDA-MB-231 cell line after nifedipine treatment. Interestingly, after nifedipine treatment migration was not significantly affected in any of tested cell lines after NCX1 silencing. Due to IP3R1 silencing, significant decrease in migration occurred in MDA-MB-231 cells after nifedipine treatment, but not in other tested cells. These results support different function of the NCX1 and IP3R1 in the invasiveness of various cancer cells due to nifedipine treatment.

Biochemical Pharmacology (Amsterdam, Netherlands) published new progress about Apoptosis. 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, Computed Properties of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Santos, S. published the artcileBryophyllum pinnatum enhances the inhibitory effect of atosiban and nifedipine on human myometrial contractility: an in vitro study, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Bryophyllum atosiban nifedipine human myometrial contractility; Atosiban; Bryophyllum pinnatum; Contractility; Myometrium; Nifedipine; Preterm.

The herbal medicine Bryophyllum pinnatum has been used as a tocolytic agent in anthroposophic medicine and, recently, in conventional settings alone or as an add-on medication with tocolytic agents such as atosiban or nifedipine. We wanted to compare the inhibitory effect of atosiban and nifedipine on human myometrial contractility in vitro in the absence and in the presence of B. pinnatum press juice (BPJ). Myometrium biopsies were collected during elective Caesarean sections. Myometrial strips were placed under tension into an organ bath and allowed to contract spontaneously. Test substances alone and at concentrations known to moderately affect contractility in this setup, or in combination, were added to the organ bath, and contractility was recorded throughout the experiments Changes in the strength (measured as area under the curve (AUC) and amplitude) and frequency of contractions after the addition of all test substances were determined Cell viability assays were performed with the human myometrium hTERT-C3 and PHM1-41 cell lines. BPJ (2.5μg/mL), atosiban (0.27μg/mL), and nifedipine (3 ng/mL), moderately reduced the strength of spontaneous myometrium contractions. When BPJ was added together with atosiban or nifedipine, inhibition of contraction strength was significantly higher than with the tocolytics alone (p = 0.03 and p < 0.001, resp.). In the case of AUC, BPJ plus atosiban promoted a decrease to 48.8 ± 6.3% of initial, whereas BPJ and atosiban alone lowered it to 70.9 ± 4.7% and to 80.9 ± 4.1% of initial, resp. Also in the case of AUC, BPJ plus nifedipine promoted a decrease to 39.9 ± 4.6% of initial, at the same time that BPJ and nifedipine alone lowered it to 78.9 ± 3.8% and 71.0 ± 3.4% of initial. Amplitude data supported those AUC data. The inhibitory effects of BPJ plus atosiban and of BPJ plus nifedipine on contractions strength were concentration-dependent. None of the test substances, alone or in combination, decreased myometrial cell viability. BPJ enhances the inhibitory effect of atosiban and nifedipine on the strength of myometrial contractions, without affecting myometrium tissue or cell viability. The combination treatment of BPJ with atosiban or nifedipine has therapeutic potential. BMC Complementary and Alternative Medicine published new progress about Apoptosis. 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

Bayer, Robin published the artcileMechano-pharmacological testing of L-type Ca2+ channel modulators via human vascular celldrum model, Application In Synthesis of 21829-25-4, the main research area is verapamil antioxidant calcium channel agonist smooth muscle cell stress; Celldrum; Biomechanics; Mechanobiology; Human arterial smooth muscle cells (haSMC); Vasoconstriction; Vasopressors; Vasoactive agents.

This study aimed to establish a precise and well-defined working model, assessing pharmaceutical effects on vascular smooth muscle cell monolayer in-vitro. This study focuses on the dilative and contractive effects of L-type Ca2+ channel agonists and antagonists, resp. We analyzed the effects of Bay K8644, nifedipine and verapamil. Three different measurement modes were developed and applied to determine the most appropriate anal. technique for the study purpose. These three operation modes are called, particular time mode, long term mode and real-time mode. It was possible to quantify the biomech. response of haSMCs to the addition of vasoactive agents using CellDrum technol. Due to the supplementation of 100nM Bay K8644, the tension increased approx. 10.6% from initial tension maximum, whereas, the treatment with nifedipine and verapamil caused a significant decrease in cellular tension: 10nM nifedipine decreased the biomech. stress around 6,5% and 50nM verapamil by 2,8%, compared to the initial tension maximum Addnl., all tested measurement modes provide similar results while focusing on different anal. parameters. Conclusion: The CellDrum technol. allows highly sensitive biomech. stress measurements of cultured haSMC monolayers. The mech. stress responses evoked by the application of vasoactive calcium channel modulators were quantified functionally (N/m2). All tested operation modes resulted in equal findings, whereas each mode features operation-related data anal.

Cellular Physiology & Biochemistry published new progress about Apoptosis. 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 In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem