Category: pyridine-derivatives

Shuman, Robert T. published the artcileAn improved synthesis of homoproline and derivatives, Synthetic Route of 123811-75-6, the main research area is homoproline derivative; proline homo derivative; piperidinecarboxylic acid; benzohomoproline.

Homoproline derivatives I (R = 3-Me, 4-Me, 6-Me, 4-Et, 4-OMe, 4-CMe3) were prepared from the corresponding pyridines II in 4 steps. A key step was the treatment of N-oxides III (R = same) with Me3SiCN and Me2NCOCl in CH2Cl2 to give nitriles IV (R = same). 5,6-Benzohomoprolines V (R1 = H, Me) were also prepared

Journal of Organic Chemistry published new progress about homoproline derivative; proline homo derivative; piperidinecarboxylic acid; benzohomoproline. 123811-75-6 belongs to class pyridine-derivatives, name is 4-(tert-Butyl)picolinic acid hydrochloride, and the molecular formula is C10H14ClNO2, Synthetic Route of 123811-75-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Browne, Emer published the artcileDesign and characterisation of an amorphous formulation of nifedipine for the treatment of autonomic dysreflexia., Application In Synthesis of 21829-25-4, the main research area is HPMC; PVP; Soluplus; amorphous solid dispersion; autonomic dysreflexia; nifedipine.

OBJECTIVES: Current treatment for autonomic dysreflexia (AD) involves rupturing a liquid-filled soft capsule of nifedipine to aid rapid drug release and absorption, however, this application is not covered under the manufacturer’s license. The objective of the current work was to design a rapidly dissolving solid dosage formulation for the treatment of AD as an alternative to the off-license “”bite and swallow”” use of currently available commercial products. METHODS: Amorphous solid dispersions (ASDs) of nifedipine were prepared by spray-drying using three different polymers: hydroxypropyl methyl cellulose (HPMC), polyvinyl pyrrolidone (PVP) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus), at a 15% w/w drug loading and were formulated and compressed into tablets. Dissolution testing was performed in the paddle dissolution apparatus using either a monophasic or biphasic medium. KEY FINDINGS: The PVP-nifedipine ASD tablets exhibited rapid dissolution, with 35% of the total nifedipine dose dissolving within 15 min in the monophasic dissolution medium. The HPMC-nifedipine ASD exhibited a very slow dissolution, while the Solupus-nifedipine system exhibited no nifedipine release over 120 min. When tested in the biphasic dissolution medium, the PVP-nifedipine ASD tablets exhibited a release profile comparable to that of the pre-split/ruptured nifedipine soft capsule product. CONCLUSIONS: This study demonstrates that a nifedipine-PVP ASD is a promising formulation strategy in the treatment of AD.

The Journal of pharmacy and pharmacology published new progress about HPMC; PVP; Soluplus; amorphous solid dispersion; autonomic dysreflexia; nifedipine. 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

Adebayo, Joshua Adeniyi published the artcileEfficacy of nifedipine versus hydralazine in the management of severe hypertension in pregnancy: A randomised controlled trial., HPLC of Formula: 21829-25-4, the main research area is Hydralazine; nifedipine; pregnancy; severe hypertension.

BACKGROUND: Despite the availability of effective antihypertensive drugs, the quality of evidence regarding the best antihypertensive agent for the treatment of hypertensive emergencies in pregnancy is still poor. AIM: The aim of this study was to compare the efficacy and side effects of oral nifedipine and intravenous hydralazine for control of blood pressure (BP) in severe hypertension in pregnancy. MATERIALS AND METHODS: An open-label, parallel, randomised, controlled trial of 78 pregnant women (â‰?8 weeks’ gestation) with severe hypertension was conducted. Severe hypertension was defined as systolic BP of 160 mmHg or above and/or diastolic BP of 110 mmHg or above. They were randomly (1:1 ratio) administered oral nifedipine 20 mg or intravenous hydralazine 10 mg every 30 min up to 5 doses or until the target BP of 140-150 mmHg systolic and 90-100 mmHg diastolic was achieved. Intravenous labetalol was given if the primary treatment failed. The primary outcome measure was the number of doses needed to achieve targeted BP. The secondary outcome measures were the time needed to achieve desired BP, maternal adverse effects and perinatal outcome. RESULTS: The sociodemographic characteristics did not differ between the two study groups. The average number of dosages (nifedipine; 1.4 ± 0.6 vs. hydralazine; 1.7 ± 0.5, P = 0.008) needed to control the BP was lower in the nifedipine arm. Time (min) taken to control the BP was similar between the groups (hydralazine; 43.7 ± 19.7 vs. nifedipine; 51.2 ± 18.9, P = 0.113). Adverse maternal and perinatal effects did not differ in the study groups. CONCLUSION: Oral nifedipine and intravenous hydralazine showed comparable efficacy in the BP control in the severe hypertensive disorders of pregnancy without significant difference in adverse maternal and perinatal outcomes. However, further studies are required to explore the role of these drugs in BP control during hypertensive emergencies in pregnancy. CLINICALTRIALS.GOV: (Identification number: NCT04435210).

The Nigerian postgraduate medical journal published new progress about Hydralazine; nifedipine; pregnancy; severe hypertension. 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

van de Vusse, Dylan published the artcilePharmacokinetics of the most commonly used antihypertensive drugs throughout pregnancy methyldopa, labetalol, and nifedipine: a systematic review, Category: pyridine-derivatives, the main research area is Hypertension; Hypertensive disorders of pregnancy; Labetalol; Methyldopa; Nifedipine; Pharmacokinetics; Pregnancy.

Abstract: Purpose: Antihypertensive drugs are among the most prescribed drugs during pregnancy. Methyldopa, labetalol, and nifedipine have been perceived safe to use during pregnancy and are therefore recommended in international guidelines for treatment of hypertension. In this review, we provide a complete overview of what is known on the pharmacokinetics (PK) of the antihypertensive drugs methyldopa, labetalol, and nifedipine throughout pregnancy. Methods: A systematic search was performed to retrieve studies on the PK of methyldopa, labetalol, and nifedipine used throughout pregnancy. The search was restricted to English and original studies. The systematic search was conducted on July 27, 2021, in Embase, Medline Ovid, Web of Science, Cochrane Library, and Google Scholar. Keywords were methyldopa, labetalol, nifedipine, pharmacokinetics, pregnancy, and placenta. Results: A total of 1459 unique references were identified of which title and abstract were screened. Based on this screening, 67 full-text papers were assessed, to retain 30 PK studies of which 2 described methyldopa, 12 labetalol, and 16 nifedipine. No fetal accumulation is found for any of the antihypertensive drugs studied. Conclusion: We conclude that despite decades of prescribing methyldopa, labetalol, and nifedipine throughout pregnancy, descriptions of their PK during pregnancy are hampered by a large heterogeneity in the low number of available studies. Aiming for evidence-based and personalized dosing of antihypertensive medication in the future, further studies on the relationship of both PK and pharmacodynamics (including the optimal blood pressure targeting) during pregnancy and pregnancy-related pathol. are urgently needed to prevent undertreatment, overtreatment, and side effects.

European Journal of Clinical Pharmacology published new progress about Hypertension; Hypertensive disorders of pregnancy; Labetalol; Methyldopa; Nifedipine; Pharmacokinetics; Pregnancy. 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

Miller, Michael J published the artcileImplementation of a standardized nurse initiated protocol to manage severe hypertension in pregnancy., Product Details of C17H18N2O6, the main research area is Hypertension; hypertensive disorders of pregnancy; patient safety; quality improvement; standardization.

Objectives: Hypertensive disorders of pregnancy are a leading cause of maternal morbidity and mortality, studies have shown that standardized protocols for treating severe hypertension improves outcomes. Our goal was to examine the effects of a protocol for treating severe hypertension.Methods: Using quality improvement methodology, we developed an evidence-based nurse-initiated protocol for management of severe hypertension. We used a before and after study design, with the primary outcome of time to administration of antihypertensive medications and time to achieve blood pressure control. Secondary outcomes included medication usage, time to repeat blood pressure, and proportion of women receiving appropriate treatment. Statistical analysis was completed with Stata, using data medians, 95% confidence intervals and a rank-sum test.Results: Data was collected for 5 months before and 5 months after protocol implementation, with 67 patients included before and 125 patients after implementation. The median time to treatment of severe range blood pressure decreased from 25 min before to 11 min after protocol implementation, pâ€?.001. Twenty-four% of women were treated within 15 min before and 60.6% were treated within 15 min after protocol implementation. Median time required to regain sustained mild range blood pressure was reduced from 45 min before to 41 min after protocol implementation, p = .004. 67.5% of women regained mild range blood pressure within 60 min before and 81.9% achieved blood pressure control within 60 min after protocol implementation. These improved outcomes were evident within the first month after protocol implementation and remained stable throughout the follow-up period.Discussion: Implementation of an evidence-based nurse-initiated protocol for the treatment of severe hypertension in pregnancy decreases the time required to administer antihypertensive medication, time required to regain blood pressure control and nonbeneficial clinical variation. In addition, these benefits were achieved rapidly within a large hospital setting.

The journal of maternal-fetal & neonatal medicine published new progress about Hypertension; hypertensive disorders of pregnancy; patient safety; quality improvement; standardization. 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, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reddy, Snigdha published the artcileHypertension and Pregnancy: Management and Future Risks., Synthetic Route of 21829-25-4, the main research area is Hypertension; Preeclampsia; Pregnancy.

Pregnancy-induced hypertension is a major cause of maternal and fetal morbidity and mortality. The overall strategies of defining and managing these conditions are aimed at preventing cardiovascular and cerebrovascular complications in the mother without jeopardizing fetal well-being. Our understanding of the origin of these disorders is evolving. Women with chronic hypertension should undergo a prepregnancy evaluation and close monitoring during and after pregnancy to ensure medication safety and to prevent end-organ damage. Based on available data, the current recommendation is that antihypertensive therapy should be initiated only in women with severe hypertension (defined as systolic blood pressure â‰?60 mm Hg and/or diastolic blood pressure â‰?05 mm Hg). It is now becoming more and more clear that hypertensive complications during pregnancy are potentially linked to cardiovascular, kidney, and metabolic diseases later in life. This review discusses the spectrum of hypertensive disorders of pregnancy, general management principles, and the need to monitor for long-term cardiovascular sequelae for decades afterward.

Advances in chronic kidney disease published new progress about Hypertension; Preeclampsia; Pregnancy. 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, Synthetic Route of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kawabata, Hideaki published the artcileIgG4-related Autoimmune Hepatitis with a Suspected Drug-induced Etiology., Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is IgG4; autoimmune hepatitis; drug-induced.

A 69-year-old man was referred to our department with acute hepatitis. He had been newly treated with benidipine hydrochloride for two months. His blood test results were as follows: aspartate aminotransferase, 1,614 IU/L; alanine aminotransferase, 1,091 IU/L and anti-smooth muscle antibody, ×80. Needle liver biopsy specimen showed interface hepatitis with mainly lymphocytic infiltration and bridging fibrosis in the periportal area. Immunohistochemistry revealed lymphocytic infiltration positive for IgG4. We diagnosed him with IgG4-related AIH with an etiology that was suspected of being drug-induced. Oral prednisolone was started and then tapered after achieving biochemical remission. Hepatitis recurred after the cessation of steroids; however, remission was achieved with ursodeoxycholic acid.

Internal medicine (Tokyo, Japan) published new progress about IgG4; autoimmune hepatitis; drug-induced. 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

Sikimic, Jelena published the artcilePossible New Strategies for the Treatment of Congenital Hyperinsulinism., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is KATP channels; KCa3.1 channels; L-type Ca2+ channels; NN414; congenital hyperinsulinism; diazoxide.

Objective: Congenital hyperinsulinism (CHI) is a rare disease characterized by persistent hypoglycemia as a result of inappropriate insulin secretion, which can lead to irreversible neurological defects in infants. Poor efficacy and strong adverse effects of the current medications impede successful treatment. The aim of the study was to investigate new approaches to silence β-cells and thus attenuate insulin secretion. Research Design and Methods: In the scope of our research, we tested substances more selective and more potent than the gold standard diazoxide that also interact with neuroendocrine ATP-sensitive K+ (KATP) channels. Additionally, KATP channel-independent targets as Ca2+-activated K+ channels of intermediate conductance (KCa3.1) and L-type Ca2+ channels were investigated. Experiments were performed using human islet cell clusters isolated from tissue of CHI patients (histologically classified as pathological) and islet cell clusters obtained from C57BL/6N (WT) or SUR1 knockout (SUR1-/-) mice. The cytosolic Ca2+ concentration ([Ca2+]c) was used as a parameter for the pathway regulated by electrical activity and was determined by fura-2 fluorescence. The mitochondrial membrane potential (ΔΨ) was determined by rhodamine 123 fluorescence and single channel currents were measured by the patch-clamp technique. Results: The selective KATP channel opener NN414 (5 µM) diminished [Ca2+]c in isolated human CHI islet cell clusters and WT mouse islet cell clusters stimulated with 10 mM glucose. In islet cell clusters lacking functional KATP channels (SUR1-/-) the drug was without effect. VU0071063 (30 µM), another KATP channel opener considered to be selective, lowered [Ca2+]c in human CHI islet cell clusters. The compound was also effective in islet cell clusters from SUR1-/- mice, showing that [Ca2+]c is influenced by additional effects besides KATP channels. Contrasting to NN414, the drug depolarized ΔΨ in murine islet cell clusters pointing to severe interference with mitochondrial metabolism. An opener of KCa3.1 channels, DCEBIO (100 µM), significantly decreased [Ca2+]c in SUR1-/- and human CHI islet cell clusters. To target L-type Ca2+ channels we tested two already approved drugs, dextromethorphan (DXM) and simvastatin. DXM (100 µM) efficiently diminished [Ca2+]c in stimulated human CHI islet cell clusters as well as in stimulated SUR1-/- islet cell clusters. Similar effects on [Ca2+]c were observed in experiments with simvastatin (7.2 µM). Conclusions: NN414 seems to provide a good alternative to the currently used KATP channel opener diazoxide. Targeting KCa3.1 channels by channel openers or L-type Ca2+ channels by DXM or simvastatin might be valuable approaches for treatment of CHI caused by mutations of KATP channels not sensitive to KATP channel openers.

Frontiers in endocrinology published new progress about KATP channels; KCa3.1 channels; L-type Ca2+ channels; NN414; congenital hyperinsulinism; diazoxide. 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

Furukawa, Naomichi published the artcileSelective ipso-substitution in pyridine ring and its application for the synthesis of macrocycles containing both oxa and thia bridges, Formula: C7H8ClNO, the main research area is macrocycle oxa thio bridge; pyridine sulfinyl sulfonyl ipso substitution; sulfonylpyridine ipso substitution; sulfonylpyridine.

Both the sulfinyl and sulfonyl groups directly bound to 2 or 4 position in pyridine were readily displaced by several nucleophiles such as RO- and RS- (R = alkyl, benzyl). The facility of the leaving groups is RSO2 �RSO > Br �Cl �RS. The ipso-substitution could be applied for the synthesis of new type of 2,6-disubstituted macrocycles I (n = 1, 2, 3) in moderate yields.

Tetrahedron Letters published new progress about macrocycle oxa thio bridge; pyridine sulfinyl sulfonyl ipso substitution; sulfonylpyridine ipso substitution; sulfonylpyridine. 42144-78-5 belongs to class pyridine-derivatives, name is 2-Chloro-6-ethoxypyridine, and the molecular formula is C7H8ClNO, Formula: C7H8ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bernard, Sylvain published the artcileEfficient synthesis of nevirapine analogs to study its metabolic profile by click fishing, HPLC of Formula: 133627-45-9, the main research area is nevirapine analog preparation azide coupling click.

Knowledge of the biotransformation and pharmacokinetics of the antiretroviral agent nevirapine is still insufficient. In order to trace rash inducing metabolites of nevirapine, a short and efficient multi-gram synthesis of a nevirapine analog that can be coupled to azide containing compounds by click chem. was developed.

Bioorganic & Medicinal Chemistry Letters published new progress about nevirapine analog preparation azide coupling click. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, HPLC of Formula: 133627-45-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem