Category: pyridine-derivatives

Ismail, Mai S. published the artcileDevelopment and assessment of oral nifedipine colloidal provesicles, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is review nifedipine colloidal provesicle assessment development.

Nifedipine(NIF), a well-known calcium channel blocker, is used in the management of hypertension especially if concomitant with kidney, heart or hormonal disorders in children. Colloidal vesicular systems were reported to improve oral absorption and bioavailability of hydrophobic drugs, so the current work embodies a new type of liquid oral colloidal provesicular nano-carrier of NIF. It was developed by simple slurry method. The optimum composition of appropriate lipid film, the effect of surfactant HLB values and cholesterol level on the entrapment efficiency of NIF within liberated vesicles were studied. Addnl., investigating the effect of both initial amount of NIF and the total lipid contents on NIF vesicular entrapment and drug loading were assessed. The morphol. and particle size of both provesicles and liberated nano-vesicles were estimated microscopically and by TEM. The study revealed that 300μmol total lipids of Span 20 /cholesterol at (9:1) molar ratio is an optimum lipid film for higher NIF encapsulation. The vesicular size attained was 209 nm and 79% EE. The in-vitro release study at pH 6.8 revealed an extended release pattern controlling both the release rate and extent. Furthermore, The DSC study showed The successful of intercalating NIF within the vesicle bilayer. This indicate the ability of these provesicles to load NIF successfully.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about Absorption. 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, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Asano, Satoshi published the artcileA new intestinal model for analysis of drug absorption and interactions considering physiological translocation of contents, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is midazolam drug absorption interaction intestinal model pharmacotherapy.

Precise prediction of drug absorption is key to the success of new drug development and efficacious pharmacotherapy. In this study, we developed a new absorption model, the advanced translocation model (ATOM), by extending our previous model, the translocation model. ATOM reproduces the translocation of a substance in the intestinal lumen using a partial differential equation with variable dispersion and convection terms to describe natural flow and micromixing within the intestine under not only fasted but also fed conditions. In comparison with ATOM, it was suggested that a conventional absorption model, advanced compartmental absorption and transit model, tends to underestimate micromixing in the upper intestine, and it is difficult to adequately describe movements under the fasted and fed conditions. ATOM explains the observed nonlinear absorption of midazolam successfully, with a minimal number of scaling factors. Furthermore, ATOM considers the apical and basolateral membrane permeabilities of enterocytes sep. and assumes compartmentation of the lamina propria, including blood vessels, to consider intestinal blood flow appropriately. ATOM estimates changes in the intestinal availability caused by drug interaction associated with inhibition of CYP3A and P-glycoprotein in the intestine. Addnl., ATOM can estimate the drug absorption in the fed state considering delayed intestinal drug flow. Therefore, ATOM is a useful tool for the anal. of local pharmacokinetics in the gastrointestinal tract, especially for the estimation of nonlinear drug absorption, which may involve various interactions with intestinal contents or other drugs.

Drug Metabolism & Disposition published new progress about Absorption. 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 of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yi, Hanxi published the artcileEvaluation of a modified flow-through method for predictive dissolution and in vitro/in vivo correlations of immediate release and extended release formulations, Category: pyridine-derivatives, the main research area is dissolution modified flow predictive method immediate extended release formulation.

The present study evaluated the ability of a modified flow-through method for predicting in vivo performance of immediate release (IR) and extended release (ER) formulations. In vitro dissolution of two model drugs, paracetamol IR tablets and felodipine ER tablets, was investigated under tuned conditions using the modified flow-through method and compared with the compendial quality control (QC) basket method. The in vivo absorption properties of paracetamol IR tablets and felodipine ER tablets were investigated in healthy volunteers. In vitro-in vivo correlation (IVIVC) anal. was performed based on the obtained in vitro and in vivo data. Our results demonstrated that the compendial QC method was not able to reflect in vivo actual absorption, while satisfactory discriminatory power and comparable in vitro dissolution/in vivo absorption were achieved for both paracetamol IR tablets and felodipine ER tablets by the modified flow-through method. This study indicated that the modified flow-through method is a potential tool to reflect in vivo performance of the IR and ER formulations.

Journal of Nanomaterials published new progress about Absorption. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Abuhassan, Qamar published the artcileStructured solubility behaviour in bioequivalent fasted simulated intestinal fluids, Quality Control of 72509-76-3, the main research area is bioequivalent fasted simulated intestinal fluid solubility.

Drug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that covered over 90% of the compositional variability. These media have been applied in this study to examine the equilibrium solubility of twenty one exemplar drugs (naproxen, indomethacin, phenytoin, zafirlukast, piroxicam, ibuprofen, mefenamic acid, furosemide, aprepitant, carvedilol, tadalafil, dipyridamole, posaconazole, atazanavir, fenofibrate, felodipine, griseofulvin, probucol, paracetamol, acyclovir and carbamazepine) to determine if consistent solubility behavior was present. The bioequivalent media provide in the majority of cases structured solubility behavior that is consistent with physicochem. properties and previous solubility studies. For the acidic drugs (pKa < 6.3) solubility is controlled by media pH, the profile is identical and consistent and the lowest and highest pH media identify the lowest and highest solubility in over 70% of cases. For weakly acidic (pKa > 8), basic and neutral drugs solubility is controlled by a combination of media pH and total amphiphile concentration (TAC), a consistent solubility behavior is evident but with variation related to individual drug interactions within the media. The lowest and highest pH x TAC media identify the lowest and highest solubility in over 78% of cases. A subset of the latter category consisting of neutral and drugs non-ionised in the media pH range have been identified with a very narrow solubility range, indicating that the impact of the simulated intestinal media on their solubility is minimal. Two drugs probucol and atazanavir exhibit unusual behavior. The study indicates that the use of two appropriate bioequivalent fasted intestinal media from the nine will identify in vitro the maximum and min. solubility boundaries for drugs and due to the media derivation this is probably applicable in vivo. These media could be applied during discovery and development activities to provide a solubility range, which would assist placement of the drug within the BCS/DCS and rationalise drug and formulation decisions.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Absorption. 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

Hu, H. published the artcileEngineering of a spider peptide via conserved structure-function traits optimizes sodium channel inhibition in vitro and anti-nociception in vivo, SDS of cas: 21829-25-4, the main research area is spider peptide conserved structure function sodium channel inhibition antinociception; chronic pain; neurological diseases; optimization; peptide engineering; rational design; sodium channel; spider peptide; therapy.

Venom peptides are potent and selective modulators of voltage-gated ion channels that regulate neuronal function both in health and in disease. We previously identified the spider venom peptide Tap1a from the Venezuelan tarantula Theraphosa apophysis that targeted multiple voltage-gated sodium and calcium channels in visceral pain pathways and inhibited visceral mechano-sensing neurons contributing to irritable bowel syndrome. In this work, alanine scanning and domain activity anal. revealed Tap1a inhibited sodium channels by binding with nanomolar affinity to the voltage-sensor domain II utilizing conserved structure-function features characteristic of spider peptides belonging to family NaSpTx1. In order to speed up the development of optimized NaV-targeting peptides with greater inhibitory potency and enhanced in vivo activity, we tested the hypothesis that incorporating residues identified from other optimized NaSpTx1 peptides into Tap1a could also optimize its potency for NaVs. Applying this approach, we designed the peptides Tap1a-OPT1 and Tap1a-OPT2 exhibiting significant increased potency for NaV1.1, NaV1.2, NaV1.3, NaV1.6 and NaV1.7 involved in several neurol. disorders including acute and chronic pain, motor neuron disease and epilepsy. Tap1a-OPT1 showed increased potency for the off-target NaV1.4, while this off-target activity was absent in Tap1a-OPT2. This enhanced potency arose through a slowed off-rate mechanism. Optimized inhibition of NaV channels observed in vitro translated in vivo, with reversal of nocifensive behaviors in a murine model of NaV-mediated pain also enhanced by Tap1a-OPT. Mol. docking studies suggested that improved interactions within loops 3 and 4, and C-terminal of Tap1a-OPT and the NaV channel voltage-sensor domain II were the main drivers of potency optimization. Overall, the rationally designed peptide Tap1a-OPT displayed new and refined structure-function features which are likely the major contributors to its enhanced bioactive properties observed in vivo. This work contributes to the rapid engineering and optimization of potent spider peptides multi-targeting NaV channels, and the research into novel drugs to treat neurol. diseases.

Frontiers in Molecular Biosciences published new progress about Acute pain. 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, SDS of cas: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mayer, Joachim M. published the artcileDeviations in the log P (partition coefficient) of protonated arylalkylamines and in their apparent log P, COA of Formula: C7H11ClN2, the main research area is amine aryl protonated partition coefficient; pyridylamine partition coefficient; phenylalkylamine partition coefficient.

Partition coefficients of monoprotonated phenyl- and 2-, 3-, and 4-pyridyl-substituted alkylamines show unpredictable but consistent trends. The coefficients of the Me, Bu, and pentyl homologs in each series are linearly related, while the Et and Pr derivatives appear too lipophilic. Thus, these partition coefficients are affected by perturbative effects, e.g., hydration or ion pairing. Also, the phosphate buffers yield abnormally low partition coefficient values.

European Journal of Medicinal Chemistry published new progress about Additivity. 84359-16-0 belongs to class pyridine-derivatives, name is 2-(Pyridin-3-yl)ethanamine hydrochloride, and the molecular formula is C7H11ClN2, COA of Formula: C7H11ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zadymova, N. M. published the artcileAdsorption of a Lipophilic Drug, Felodipine, at Different Interfaces, COA of Formula: C18H19Cl2NO4, the main research area is adsorption lipophilic drug felodipine different interface.

In connection with the development of methods for the delivery of lipophilic drugs in a bioavailable form, we have employed an integrated approach to the investigation of the adsorption of an antihypertensive drug, felodipine, at interfaces that simulate the surfaces of different carriers. Isotherms have been plotted for felodipine adsorption from solutions in heptane (C = 2.13 x 10-5 – 4.26 x 10-4 M) at interfaces with water and silver metal, as well as for the compression of drug monolayers formed on a water surface from the heptane solutions The quant. characteristics of the studied felodipine layers have been determined, and their phase state and the most probable conformation of adsorbed drug mols. have been analyzed taking into account the data of mol. dynamics simulations. The phase state of the felodipine layers at the heptane/water interface is adequately described by the van Laar equation. A bilayer is formed at the silver surface. A phase transition from a gaseous state to a liquid-expanded state has been revealed for the felodipine layers.

Colloid Journal published new progress about Adsorption. 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, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Palmquist, Karl H. published the artcileReciprocal cell-ECM dynamics generate supracellular fluidity underlying spontaneous follicle patterning, Quality Control of 21829-25-4, the main research area is supracellular fluidity extracellular matrix follicle cell; active soft matter; biophysics; contractility; emergence; extracellular matrix; mechanics; mechanosensation; morphogenesis; multicellular; organogenesis; periodic patterning; self-organization; skin.

During vertebrate embryogenesis, cell collectives engage in coordinated behavior to form tissue structures of increasing complexity. In the avian skin, assembly into follicles depends on intrinsic mech. forces of the dermis, but how cell mechanics initiate pattern formation is not known. Here, we reconstitute the initiation of follicle patterning ex vivo using only freshly dissociated avian dermal cells and collagen. We find that contractile cells phys. rearrange the extracellular matrix (ECM) and that ECM rearrangement further aligns cells. This exchange transforms a mech. unlinked collective of dermal cells into a continuum, with coherent, long-range order. Combining theory with experiment, we show that this ordered cell-ECM layer behaves as an active contractile fluid that spontaneously forms regular patterns. Our study illustrates a role for mesenchymal dynamics in generating cell-level ordering and tissue-level patterning through a fluid instability-processes that may be at play across morphol. symmetry-breaking contexts.

Cell (Cambridge, MA, United States) published new progress about Aggregates. 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

Schmidt, Michael A. published the artcileEffect of Terminal Alkylation of Aryl and Heteroaryl Hydrazines in the Fischer Indole Synthesis, Computed Properties of 3469-63-4, the main research area is Fischer indole synthesis; hydrazine ketone alkylation amidation cross coupling.

The effect of alkylation on the terminal position of aryl and heteroaryl hydrazines in the Fischer indole synthesis was examined Compared to their unalkylated counterparts, reactions using alkylated s provided indole products with higher yields and faster rates. The reactions can be conducted at lower temperatures and are compatible with acid-sensitive functionality. The terminally alkylated hydrazines were readily prepared by a new two-step sequence and held as stable hydrazinium salts. The mild formation of the salts along with the favorable Fischer indole reaction conditions highlights the potential of this approach in later-stage synthetic use.

Journal of Organic Chemistry published new progress about Alkylation. 3469-63-4 belongs to class pyridine-derivatives, name is Ethyl 5-methoxy-1H-pyrrolo[2,3-c]pyridine-2-carboxylate, and the molecular formula is C11H12N2O3, Computed Properties of 3469-63-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lamberto, Massimiliano published the artcileMicrowave-assisted synthesis of symmetric and asymmetric viologens, SDS of cas: 36437-30-6, the main research area is sym asym viologen microwave assisted synthesis.

Viologens are generally synthesized by N-alkylating 4,4′-bipyridine with alkyl halides. Under conventional heating conditions, however, their synthesis suffers from long reaction times and, often, low yields. In this work, sym. and asym. viologens were synthesized under the assistance of microwave irradiation in good to excellent yields and in short reaction times.

Tetrahedron Letters published new progress about Alkylation. 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, SDS of cas: 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem