Category: pyridine-derivatives

Cao, Dawei published the artcileLight-driven transition-metal-free direct decarbonylation of unstrained diaryl ketones via a dual C-C bond cleavage, Formula: C12H9NO, the publication is Nature Communications (2022), 13(1), 1805, database is CAplus and MEDLINE.

An efficient light-driven transition-metal-free strategy for decarbonylation of unstrained diaryl ketones R¹C(O)R² (R¹ = Ph, 2H-1,3-benzodioxol-5-yl, thiophen-2-yl, etc.; R² = Ph, 4-methoxyphenyl, pyridin-2-yl, etc.) to construct biaryl compounds R¹R² through dual inert C – C bonds cleavage was reported. This reaction featured mild reaction conditions, easy-to-handle reactants and reagents, and excellent functional groups tolerance. The mechanistic investigation and DFT calculation suggest that this strategy proceeds through the formation of dioxy radical intermediate via a single-electron-transfer (SET) process between photo-excited diaryl ketone and DBU mediated by DMSO, followed by removal of CO₂ to construct biaryl compounds

Nature Communications published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C12H9NO, Formula: C12H9NO.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Law, Robert P. published the artcileDiscovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain, Safety of 3-Methoxypyridine-4-boronic acid, the publication is Journal of Medicinal Chemistry (2018), 61(10), 4317-4334, database is CAplus and MEDLINE.

The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains-BRD2, BRD3, BRD4, and BRDT-each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biol. function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochem. properties, culminating in potent BET inhibitors with BD2 selectivity.

Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Safety of 3-Methoxypyridine-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Law, Robert P. published the artcileDiscovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain, Quality Control of 844501-00-4, the publication is Journal of Medicinal Chemistry (2018), 61(10), 4317-4334, database is CAplus and MEDLINE.

The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains-BRD2, BRD3, BRD4, and BRDT-each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biol. function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochem. properties, culminating in potent BET inhibitors with BD2 selectivity.

Journal of Medicinal Chemistry published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Quality Control of 844501-00-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lopez-Alvarado, Pilar published the artcileA general synthesis of quinoline-2,5,8(1H)-triones via acylation of 2,5-dimethoxyaniline with S-tert-butyl thioacetates by application of the Knorr cyclization, Synthetic Route of 107263-95-6, the publication is Synthesis (1998), 186-194, database is CAplus.

An efficient synthesis of 3- and/or 4-alkylated quinoline-2,5,8(1H)-triones is described. The reaction sequence employed involves Knorr cyclization of 2,5-dimethoxyanilides into 5,8-dimethoxyquinoline systems, followed by oxidative demethylation with (NH₄)₂Ce(NO₃)₆. The starting 2,5-dimethoxyanilides were prepared by chemoselective acylation of 2,5-(MeO)₂C₆H₃NH₂ with a series of β-oxo thioesters obtained by regioselective alkylation of AcCH₂C(O)SCMe₃ at C(2) and/or C(4). The introduction of electrophiles other than alkyl groups at C(2) on AcCH₂C(O)SCMe₃ was also studied.

Synthesis published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C6H5F4NO3S, Synthetic Route of 107263-95-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yamada, Masatoshi published the artcileHighly Enantioselective Direct Asymmetric Reductive Amination of 2-Acetyl-6-Substituted Pyridines, Synthetic Route of 91-02-1, the publication is Organic Letters (2021), 23(9), 3364-3367, database is CAplus and MEDLINE.

A highly direct asym. reductive amination of a variety of ketone substrates, including 2-acetyl-6-substituted pyridines, β-keto esters, β-keto amides, and 1-(6-methylpyridin-2-yl)propan-2-one, has been disclosed for the first time (94.6% to >99.9% ee). With ammonium trifluoroacetate as the nitrogen source, various chiral corresponding primary amines were prepared in excellent enantioselectivity and conversion in the presence of a com. available and inexpensive chiral catalyst, Ru(OAc)₂{(S)-binap}, under 0.8 MPa of hydrogen gas pressure.

Organic Letters published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C10H18BNO4, Synthetic Route of 91-02-1.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Peeters, Laura E. J. published the artcileDevelopment and Validation of a Dried Blood Spot Assay Using UHPLC-MS/MS to Identify and Quantify 12 Antihypertensive Drugs and 4 Active Metabolites: Clinical Needs and Analytical Limitations, Formula: C17H18N2O6, the publication is Therapeutic Drug Monitoring (2022), 44(4), 568-577, database is CAplus and MEDLINE.

As nonadherence to antihypertensive drugs (AHDs) can increase the risk of cardiovascular events, hospitalization, and higher costs, there is a need for a reliable, objective, and easy method to assess nonadherence in patients. The dried blood spot (DBS) sampling method used to measure drug concentrations meets these requirements. For detecting nonadherence, identification is more important than quantification. Owing to their use in clin. practice, it is important to measure multiple AHDs with a single method. Therefore, we developed and validated a single DBS method for 17 commonly used AHDs and 4 active metabolites using ultrahigh performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS). Anal. validation of the DBS assay was performed in accordance with the guidelines on bioanal. method validation of the European Medicines Agency and US Food and Drug Administration as well as the International Association of Therapeutic Drug Monitoring and Clin. Toxicol. guidelines. We validated 12 of the 17 AHDs according to the European Medicines Agency and Food and Drug Administration requirements for bioanal. method validation. Eleven AHDs were validated for both identification and quantification of drug concentrations, whereas nifedipine was only validated for identification. However, 5 of the 17 AHDs were excluded due to suboptimal validation results. Lercanidipine was excluded due to nonlinearity, and all 4 AHDs measured in the neg. mode of UHPLC-MS/MS were not in accordance with one or more of the acceptance criteria and were therefore excluded. The described method accurately measured AHDs in DBS and can be used to determine nonadherence in patients. However, method validation revealed a challenging balance between anal. limitations and clin. needs when analyzing multiple drugs using the same method.

Therapeutic Drug Monitoring published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Formula: C17H18N2O6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Empel, Anna published the artcileTowards Property Profiling: SYNTHESIS and SAR Probing of New Tetracyclic Diazaphenothiazine Analogues, Synthetic Route of 39856-58-1, the publication is International Journal of Molecular Sciences (2021), 22(23), 12826, database is CAplus and MEDLINE.

A series of new tertiary phenothiazine derivatives containing a quinoline and a pyridine fragment was synthesized by the reaction of 1-methyl-3-benzoylthio-4-butylthioquinolinium chloride with 3-aminopyridine derivatives bearing various substituents on the pyridine ring. The direction and mechanism of the cyclization reaction of intermediates with the structure of 1-methyl-4-(3-pyridyl)aminoquinolinium-3-thiolate was related to the substituents in the 2- and 4-pyridine position. The structures of the compounds were analyzed using 1H, 13C NMR (COSY, HSQC, HMBC) and X-ray anal., resp. Moreover, the antiproliferative activity against tumor cells (A549, T47D, SNB-19) and a normal cell line (NHDF) was tested. The antibacterial screening of all the compounds was conducted against the reference and quality control strain Staphylococcus aureus ATCC 29213, three clin. isolates of methicillin-resistant S. aureus (MRSA). In silico computation of the intermol. similarity was performed using principal component anal. (PCA) and hierarchical clustering anal. (HCA) on the pool of structure/property-related descriptors calculated for the novel tetracyclic diazaphenothiazine derivatives The distance-oriented property evaluation was correlated with the exptl. anticancer activities and empirical lipophilicity as well. The quant. shape-based comparison was conducted using the CoMSA method in order to indicate the potentially valid steric, electronic and lipophilic properties. Finally, the numerical sampling of similarity-related activity landscape (SALI) provided a subtle picture of the SAR trends.

International Journal of Molecular Sciences published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Synthetic Route of 39856-58-1.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Teimouri, Arezou published the artcileStability of Compounded Topical Nifedipine in Cream, Gel, and Ointment Bases., HPLC of Formula: 21829-25-4, the main research area is .

The objective of this study was to investigate the stability of compounded nifedipine cream in gel and ointment formulations dispensed in white plastic and glass amber jars. Extemporaneously compounded nifedipine cream (Glaxal Base), gel (K-Y Jelly), and ointment (Aquaphor) in white plastic and glass amber jars were stored at 4°C, 23°C, and 40°C. We determined potency on days 0, 7, 14, 30, 60, and 90, and subsequently assigned beyond-use-dates based on United States Pharmacopeia recommendations, organoleptic properties, and pH changes. Nifedipine potency in cream and ointment stored in white plastic jars was within ±10% of initial for 90 days (excluding day 14 for cream). In glass amber jars, potency was outside the acceptable range by day 14 at 23°C but within range for 90 days at 4°C (excluding day 30). Nifedipine potency was maintained for 90 days in both jars at 23°C and 4°C (excluding day 30) and in white plastic jars at 40°C, but 60 days stored in glass amber jars. The pH of formulations was stable with changes of less than 1-unit pH. At 40°C, a significant decrease in apparent viscosity of cream was evident on day 90. There was a decrease in apparent viscosity and phase separation of the ointment at 40°C and an increase in apparent viscosity (difficult to mix) at 4°C on day 14 onwards. Significant organoleptic changes were observed by day 7 at 40°C (decrease in apparent viscosity and abnormal odor by day 90), day 30 at 4°C (thicker consistency), and day 90 at 23°C (abnormal odor). Storage in white plastic jars at 23°C is recommended for compounded topical nifedipine cream and ointment (for 90 days), and for gel (60 days).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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

Teimouri, Arezou published the artcileDrug-release Assessment of Compounded Topical Nifedipine and Diltiazem in Commonly Used Bases for Wound Healing., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is .

The objective of this study was to determine release profiles of extemporaneously compounded nifedipine and diltiazem in commonly used bases in pharmacy practice. Release of nifedipine 0.2%, 2%, and 10% (w/w) from Glaxal Base, K-Y Jelly, and Aquaphor Healing Ointment, and of diltiazem 2% (w/w) from GlaxalBase, hydroxyethyl cellulose-based gel, and white petrolatum was quantified using the Franz-cell diffusion system. The cumulative release was determined at 0.5 hour, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, and 6 hours. Two-way ANOVA with Tukey’s posthoc test was used for statistical analyses, with a P-value of <0.05 considered significant. At a 0.2% concentration, cumulative nifedipine release was highest from Glaxal Base. At 2% and 10% concentrations, nifedipine release was highest from K-Y Jelly, although this was only significantly different from Glaxal Base at 6 hours and 1.5 hours, 4 hours, 6 hours (P<0.05), respectively. Diltiazem release from Glaxal Base and white petrolatum was significantly lower than the gel (P<0.05). No significant difference in diltiazem release from Glaxal Base at 0.5 hour was observed versus white petrolatum (P>0.05). Nifedipine and diltiazem release both followed Higuchi’s mathematical model with the highest coefficient of determination (R2) for all formulations. Of the bases studies, Glaxal Base is the recommended base for compounding topical nifedipine (0.2%). For higher concentrations of nifedipine (2% and10%), both Glaxal Base and K-Y Jelly are suitable options for base selection. A hydroxyethylcellulose-based gel is recommended for topical diltiazem (2%).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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

Riepl, Mike published the artcileA Compendium of Compounding Agents and Formulations, Part 4: Nifedipine and Pentoxifylline., Category: pyridine-derivatives, the main research area is .

The medical, economic, and social effects of painful chronic wounds such as anal fissures, which frequently prove refractory to treatment with commercially available medications, are often underestimated by clinicians. Those types of injuries, which afflicted individuals are often reluctant to discuss with healthcare providers, can lead to a greatly restricted lifestyle; result in depression, anxiety, social isolation, and embarrassment; require extended or repeated hospital stays; and create a financial burden for the patient and for society. Because interpatient variables can preclude the effectiveness of standardized mass-produced wound-healing products, a compounded formulation that can be formulated to include drugs proven effective in safe but off-label uses and that can be modified as patients’ medical needs require may achieve the therapeutic goal. In this report, 2 such agents shown to promote wound healing are profiled: the vasodilator nifedipine, a first-generation calcium channel blocker that is used to treat hypertension and angina pectoris; and pentoxifylline, a synthetic dimethylxanthine derivative that facilitates vasodilation, improves erythrocyte flexibility, enhances blood flow, and reduces blood viscosity. Formulations that incorporate those drugs, which are underrecognized as effective healing agents when compounded as directed, are included for easy reference.

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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