Month: December 2022

Oraebosi, Michael Ikechukwu published the artcileChronopharmacology of the alpha-lipoic acid/nifedipine/glimepiride combination in the amelioration of retinopathy in rats, Related Products of pyridine-derivatives, the main research area is nifedipine glimepiride antioxidant diabetic retinopathy; Chronopharmacolgy; alpha-lipoic acid; diabetic retinopathy; diurnal variation; glimepiride; nifedipine.

Time of drug administration affects both the kinetics and dynamics of medications. This study investigated diurnal efficacy of alpha-lipoic acid (ALA), nifedipine, and glimepiride combination in the treatment of diabetic retinopathy. The study design comprised seven groups of rats, with groups 1 and 2 serving as non-diabetic and diabetic controls, resp., receiving 1 mL/kg distilled water. All other groups were diabetic, and received 10 mg/kg glimepiride at 20:00 h. Groups 4-7 also received 20 mg/kg nifedipine at 08:00 h. In addition, groups 5-7 received 100 mg/kg ALA at 08:00 h, 14:00 h, and 20:00 h, resp. Oral drug administration was for 28 days during which fasting and random blood glucose sampling were done weekly at 07:30 h and 13:30 h, resp. On the 29th day, rats were euthanized; blood was collected via the jugular veins for determination of serum ocular markers like magnesium, cholesterol, and triglyceride. Furthermore, the eyes were excised and their relative organ/body weight ratios determined The right eyes were persevered in phosphate buffer for homogenization and determination of retina antioxidant profile (MDA, SOD, CAT, GSH), while the left eyes were preserved in formalin for histol. examination Results showed that treatment with ALA and glimepiride at 20:00 h along with nifedipine at 08:00 h resulted in better prognosis than other treatment groups and with improved glycemic control. Also, all their serum markers for retinopathy, organ weight, and histol. did not differ significantly from that of the non-diabetic rats. Findings imply that diurnal efficacy in alpha-lipoic acid, nifedipine and glimepiride combination ameliorates diabetic retinopathy in rats and may be beneficial in the treatment of diabetic retinopathy.

Chronobiology International published new progress about Antioxidants. 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Oraebosi, M. I. published the artcileDiurnal efficacy of alpha-lipoic acid/nifedipine/glimepiride combination mitigates diabetic neuropathies in rats, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is diabetic neuropathy nifedipine glimepiride; Acide alpha-lipoïque; Alpha-lipoic acid; Circadian rhythm; Diabetic neuropathies; Glimepiride; Glimépiride; Neuropathies diabétiques; Nifedipine; Nifédipine; Rythme circadien.

Time-dependent effects of alpha-lipoic acid/nifedipine/glimepiride combination on diabetic neuropathies were investigated in rats. 7 groups (n = 9) of rats were used.First and second groups were apparently normal and diabetic rats resp., and were administered 1 mL/kg distilled water. The rest of the groups were diabetic and administered 10 mg/kg glimepiride at night-time (8:00 pm). Groups 4-7 were administered addnl. 20 mg/kg nifedipine at morning-time (8:00 am), while groups 5-7 were also administered 100 mg/kg alpha-lipoic acid (ALA) in the morning, afternoon and night-time resp. (8:00 am, 2:00 pm and 8:00 pm). During the 28 days of oral treatment, paw pressure, tail immersion and motor coordination tests were conducted. The rats were euthanized on the 29th day after a charcoal meal. The small intestines were excised to determine intestinal transit while the brain was collected, homogenised and used to determine levels of oxidative stress.Data show that treatment with ALA at 8:00 am or 2:00 pm significantly (P ≤ 0.01) produced a delay in the onset and improved prognosis of neuropathies. Treatment with ALA at 8:00 pm prevented manifestation of neuropathies throughout the study with pos. antioxidant effects.Time-dependent ALA treatment in combination with nifedipine and glimepiride should be studied in humans with an approx. similar circadian timing. This may provide addnl. clin. therapeutic options for diabetic neuropathies.

Annales Pharmaceutiques Francaises published new progress about Antioxidants. 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

Xu, Lu published the artcilePLA-PEG Micelles Loaded with a Classic Vasodilator for Oxidative Cataract Prevention, Application In Synthesis of 21829-25-4, the main research area is polylactic acid PEG micelle nifedipine cataract eye; calcium channel blocker; cataract treatment; eye drop; micelles; oxidative stress.

The only treatment for cataract in clinic is the clouded lens removal combined with artificial lens implantation. In this study, nifedipine (NFP), a classic vasodilator, was loaded in a U.S. FDA-approved polymer PLA-PEG to form NFP-loaded PLA-PEG micelles as a novel eye drop to prevent oxidative cataract formation and progression at the early stage. The NFP-loaded PLA-PEG micelles not only showed satisfactory biocompatibility and bioavailability, but also efficiently improved the anticataract ability through the inhibition of extracellular calcium ions influx. This study may provide a new insight into the development of cataract treatment.

ACS Biomaterials Science & Engineering published new progress about Antioxidants. 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

Yao, Jianwen published the artcileDesign, synthesis and biological activities of sorafenib derivatives as antitumor agents, Recommanded Product: Methyl 4-chloropicolinate, the main research area is sorafenib derivative preparation antitumor antiangiogenesis activity.

A series of novel sorafenib derivatives was designed and synthesized in high yields using various substituted anilines, and their antiproliferative activities against HCT116, PC-3 and MDA-MB-231 cell lines were also evaluated and described. All compounds exhibited potent antiproliferative activity against HCT116 and PC-3 cells with IC50 = 2.8-52.0 and 2.2-45.6 μM; compounds I [R = Et, cyclopropyl] demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines; the cytotoxicity of compound I [R = cyclohexyl] is more potent than that of sorafenib. Some compounds were chosen for further evaluation of the anti-angiogenesis activity, and showed the inhibition of sprout formation from aortic ring ex vivo. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.

Bioorganic & Medicinal Chemistry Letters published new progress about Angiogenesis. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pavia, Michael R. published the artcileN,N-Disubstituted 6-alkoxy-2-pyridinamines as anticonvulsant agents, HPLC of Formula: 42144-78-5, the main research area is alkoxypyridinamine preparation anticonvulsant; chloropyridine alkoxylation; alkoxychloropyridine aminolysis piperazine piperidine morpholine; pyridinamine alkoxy preparation anticonvulsant; aminopyridine alkoxy preparation anticonvulsant.

The anticonvulsant effect of a series of title compounds I (R = Me, Et, Me2CH, Me2CHCH2, Me2NCH2CH2, cyclopropylmethyl, cyclohexyl, cyclohexylmethyl; R1 = e.g., piperazino, piperidino, morpholino) is described. The activity/side-effect ratio in this series of compounds was optimized. I (R = Me2CHCH2; R1 = piperazino) (II) showed the most desirable profile, and was selected for a more complete pharmacol. evaluation. Overall, the pharmacol. profile of II is very similar to that of diphenylhydantoin (phenytoin). While II is nearly equipotent to phenytoin, animal studies suggest a fairly short duration of action. In addition, II exhibited some troublesome side effects including central nervous system depression and hypothermia.

Journal of Medicinal Chemistry published new progress about Alkoxylation. 42144-78-5 belongs to class pyridine-derivatives, name is 2-Chloro-6-ethoxypyridine, and the molecular formula is C7H8ClNO, HPLC of Formula: 42144-78-5.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bach, Peter published the artcileEffects of the Pyridine 3-Substituent on Regioselectivity in the Nucleophilic Aromatic Substitution Reaction of 3-Substituted 2,6-Dichloropyridines with 1-Methylpiperazine Studied by a Chemical Design Strategy, SDS of cas: 132097-09-7, the main research area is effect dichloropyridine substituent regioselectivity nucleophilic aromatic substitution reaction.

A chem. design strategy has been used to select 3-substituted 2,6-dichloropyridines for the nucleophilic aromatic substitution reaction with 1-methylpiperazine. The aim was to study the dependency of the regioselectivity in these reactions on the character of the pyridine 3-substituent expressed by their lipophilicity (PI), size (MR), and inductive effect (σp). Interestingly, the regioselectivity did not correlate with any of these parameters, but in a statistically significant manner with the Verloop steric parameter B1, as indicated by the p value of 0.006 (R2 = 0.45). This implies that bulky 3-substituents close to the pyridine ring induce regioselectivity towards the 6-position. Useful in practical synthesis is the different regioselectivity obtained with a carboxylic acid 3-substituent and precursors or derivatives thereof. Thus, in acetonitrile as solvent, 3-carboxylate and 3-amide substituents were preferred to obtain the 2-isomer (9:1 ratio of the 6-isomer), whereas the 3-cyano and 3-trifluoromethyl substituents were preferred to obtain the 6-isomer (9:1 ratio of the 2-isomer). Anal. of the regioselectivity Rsel for the pyridine 2-position in the reaction of 2,6-dichloro-3-(methoxycarbonyl)pyridine with 1-methylpiperazine in 21 different solvents showed that Rsel could be predicted by the Kamlet-Taft equation: Rsel = 1.28990 + 0.03992α – 0.59417β – 0.46169π* (R2 = 0.95, p = 1.9 × 10-10). Rsel is thus mainly correlated with the ability of the solvent to function as a hydrogen-bond acceptor, as expressed by the solvatochromic β parameter. Thus, the 16:1 regioselectivity for the 2-isomer in DCM (β = 0.10) could be switched to a 2:1 selectivity for the 6-isomer in DMSO (β = 0.76).

European Journal of Organic Chemistry published new progress about Hydrogen bond. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, SDS of cas: 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Velraj, G. published the artcileInvestigation of structure, vibrational, electronic, NBO and NMR analyses of 2-chloro-4-nitropyridine (CNP), 2-chloro-4-methyl-5-nitropyridine (CMNP) and 3-amino-2-chloro-4-methylpyridine (ACMP) by experimental and theoretical approach, Synthetic Route of 133627-45-9, the main research area is chloronitropyridine chloromethylnitropyridine aminochloromethylpyridine structure vibration electronic NBO NMR analysis; 2-Chloro-4-methyl-5-nitropyridine; 2-Chloro-4-nitropyridine; 3-Amino-2-chloro-4-methylpyridine; DFT; NMR.

This study reports about the optimized mol. structures, vibrational wavenumbers, at. charges, mol. electrostatic potentials, NBO, electronic properties, 1H NMR and 13C NMR chem. shifts for the mols. 2-chloro-4-nitropyridine (CNP), 2-chloro-4-methyl-5-nitropyridine (CMNP) and 3-amino-2-chloro-4-methylpyridine (ACMP). Theor. calculations were performed by d. functional theory (DFT)/B3LYP method using 6-311++G (d,p) basis set. The stability and charge delocalization of the title mols. were studied by natural bond orbital (NBO) anal. Mol. electrostatic potential maps (MEP) were calculated to predict the reactive sites. The reactivity of the title compounds were investigated by HOMO-LUMO energies and global descriptors. The electronic properties of the compounds were also discussed and the transitions were found to be π → π*. In addition, the thermodn. properties were studied for the title compounds and corresponding relations between the properties and temperature were also discussed. The hyperpolarizability values (βtot) were calculated for the title compounds Hyperpolarizability value (βtot) of CMNP was found to be high and nineteen times greater than that of urea.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Dipole moment. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Synthetic Route of 133627-45-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Puszko, A. published the artcileElectric dipole moments of 2,4-dihalopicolines and their N-oxides, Application In Synthesis of 132097-09-7, the main research area is dipole moment picoline oxide halogen derivative.

Dipole moment values of 2,4-dichloro- and 2,4-dibromopicolines and their N-oxides were calculated from the permittivity and refractive indexes measurements as well as by means of composition of groups and bonds moments vectors. The influence of substituents effects on the dipole moment values was discussed and the results obtained were compared.

Chemical Papers published new progress about Dipole moment. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Application In Synthesis of 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Maidan, Ruben published the artcileApplication of multielectron charge relays in chemical and photochemical debromination processes. The role of induced disproportionation of N,N’-dioctyl-4,4′-bipyridinium radical cation in two-phase systems, Application of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, the main research area is disproportionation bipyridinium cation radical debromination; photochem reduction bipyridinium disproportionation.

Photochem. and chem. reduction of N,N’-dioctyl-4,4′-bipyridinium to the corresponding radical cation (I) leads to induced disproportionation of I in an aqueous-organic, 2-phase system, yielding the 2-electron reduction product II. The induced disproportionation is a result of opposite solubility properties of the disproportionation products in the 2 phases. II mediates the debromination of 1,2- and 1,1-dibromo substrates.

Journal of the American Chemical Society published new progress about Debromination. 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, Application of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Takahashi, Tamayo published the artcileComponent of nicotine-induced intracellular calcium elevation mediated through α3- and α5-containing nicotinic acetylcholine receptors are regulated by cyclic AMP in SH-SY 5Y cells, Quality Control of 21829-25-4, the main research area is nicotine nAChR cyclic AMP SH SY 5Y cell.

The pathway from the medial habenular nucleus to the interpeduncular nucleus, in which nicotinic acetylcholine receptor (nAChR) including the α3 and α5 subunits (α3 * and α5 * nAChRs) are expressed, is implicated in nicotine dependence. We investigated whether α3 * and α5 * nAChRs are regulated by cAMP using SH-SY5Y cells to clarify the significance of these receptors in nicotine dependence. We analyzed the nicotine-induced elevation of intracellular Ca2+ ([Ca2+]i). Nicotine induces a concentration-dependent increase in [Ca2+]i. The elimination of Ca2+ from extracellular fluid or intracellular stores demonstrated that the nicotine-induced [Ca2+]i elevation was due to extracellular influx and intracellular mobilization. The effects of tubocurarine on nicotine-induced [Ca2+]i elevation and current suggest that intracellular mobilization is caused by plasma membrane-permeating nicotine. The inhibition of α3 *, α5 *, α7 nAChR and voltage-gated Ca2+ channels by using siRNAs and selective antagonists revealed the involvement of these nAChR subunits and channels in nicotine-induced [Ca2+]i elevation. To distinguish and characterize the α3 * and α5 * nAChR-mediated Ca2+ influx, we measured the [Ca2+]i elevation induced by nonmembrane-permeating acetylcholine when muscarinic receptors, α7nAChR and Ca2+ channels were blocked. Under this condition, the [Ca2+]i elevation was significantly inhibited with a 48-h treatment of dibutyryl cAMP, which was accompanied by the downregulation of α3 and β4 mRNA. These findings suggest that α3 * and α5 * nAChR-mediated Ca2+ influx is possibly regulated by cAMP at the transcriptional level.

PLoS One published new progress about Cell membrane. 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