Pyridine-derivatives

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

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

Shao, Ning published the artcileSynthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H₃ antagonists, Related Products of pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(5), 2075-2078, database is CAplus and MEDLINE.

The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H₃ antagonists is described. Introduction of substituted Ph, pyridyl, and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H₃ antagonist activity in both ex vivo and in vivo assays.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C13H19Br2ClN2O, Related Products of pyridine-derivatives.

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

Rozatian, Neshat published the artcileA quantitative reactivity scale for electrophilic fluorinating reagents, Related Products of pyridine-derivatives, the publication is Chemical Science (2018), 9(46), 8692-8702, database is CAplus and MEDLINE.

The N-F reagent was currently determined through empirical experimentation in the absence of quant. values for electrophilicities. An exptl.-determined kinetic reactivity scale for ten N-F fluorinating reagents, including Selectfluor, NFSI, Synfluor and several N-fluoropyridinium salts, in CH₃CN ws reported. The reactivity scale, which covers eight orders of magnitude, employs para-substituted 1,3-diaryl-1,3-dicarbonyl derivatives to measure relative and absolute rate constants The para-substituted 1,3-diaryl-1,3-dicarbonyl scaffold delivers a convenient, sensitive spectrophotometric reporter of reactivity that also led to the discovery of a unique form of tautomeric polymorphism.

Chemical Science 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, Related Products of pyridine-derivatives.

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

Le, Song Thi published the artcileSynthesis of 2-Aryl-5-Nitropyridines by Three-Component Ring Transformation of 3,5-Dinitro-2-Pyridone, SDS of cas: 89076-64-2, the publication is Asian Journal of Organic Chemistry (2014), 3(3), 297-302, database is CAplus.

2-Arylated-5-nitropyridines were efficiently synthesized by a three-component ring transformation of 3,5-dinitro-2-pyridone with aromatic ketones in the presence of ammonium acetate wherein the dinitropyridone served as a synthetic equivalent of an unstable nitromalonaldehyde. 2,8-Diazabicyclo[3.3.1]non-3-ene derivative was formed as a byproduct and was converted into nitropyridines by heating in the presence of ammonium acetate. This exptl. fact implied that the former compound was a kinetically controlled product and the latter was a thermodynamically controlled product because of the aromatization. This eco-friendly method was applicable to various kinds of aryl and (hetero)aryl ketones to afford the corresponding (hetero)arylated pyridines in good to excellent yields.

Asian Journal of Organic Chemistry published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C11H8N2O2, SDS of cas: 89076-64-2.

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

Wendt, Ida published the artcileEffects of Five Antifouling Biocides on Settlement and Growth of Zoospores from the Marine Macroalga Ulva lactuca L., Product Details of C23H20BN, the publication is Bulletin of Environmental Contamination and Toxicology (2013), 91(4), 426-432, database is CAplus and MEDLINE.

Antifouling biocides are found in the marine ecosystem were they can affect non-target organisms. In this study the effects of five antifouling biocides on the settlement and growth of Ulva lactuca zoospores were investigated. The biocides investigated were copper (Cu²⁺), 4,5-dichloro-2-n-octyl-3(2H)-isothiazolone (DCOIT), triphenylborane pyridine (TPBP), tolylfluanid and medetomidine. Full concentration-response curves where determined for each compound EC₅₀ values were determined for copper, DCOIT, TPBP and tolylfluanid, all of which inhibited settlement and growth in a concentration dependent manner with the following toxicity ranking; tolylfluanid (EC₅₀ 80 nmol L^-1) âˆ?DCOIT (EC₅₀ 83 nmol L^-1) > TPBP (EC₅₀ 400 nmol L^-1) > Cu²⁺ (EC₅₀ 2,000 nmol L^-1). Medetomidine inhibited settlement and growth only at the extreme concentration of 100,000 nmol L^-1 (93 % effect). The low toxicity is possibly a consequence of a lack of receptors that medetomidine can bind to in the U. lactuca zoospores.

Bulletin of Environmental Contamination and Toxicology published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C25H47NO8, Product Details of C23H20BN.

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

Bandarage, Upul K. published the artcileDiscovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors, Product Details of C8H7NO, the publication is ACS Medicinal Chemistry Letters (2021), 12(1), 129-135, database is CAplus and MEDLINE.

Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. PI3Kγ plays a critical role in mediating leukocyte chemotaxis as well as mast cell degranulation, making it a potentially interesting target for autoimmune and inflammatory diseases. We previously disclosed a novel series of PI3Kγ inhibitors derived from a benzothiazole core. The truncation of the benzothiazole core led to the discovery of a structurally diverse alkynyl thiazole series which displayed high PI3Kγ potency and subtype selectivity. Further medicinal chem. optimization of the alkynyl thiazole series led to identification of compounds such as 14 and 32, highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitors. Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo.

ACS Medicinal Chemistry Letters published new progress about 1060816-39-8. 1060816-39-8 belongs to pyridine-derivatives, auxiliary class Pyridines, name is 4-Ethynyl-2-methoxypyridine, and the molecular formula is C8H7NO, Product Details of C8H7NO.

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

Carmona-Vargas, Christian C. published the artcileDetermination of the binding constants of propeller-like metal complexes of picolinaldehyde-2-pyridylhydrazone, Name: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, the publication is Inorganica Chimica Acta (2019), 275-280, database is CAplus.

Herein, the authors determined the binding constants for transition metal complexes of Cu²⁺, Co²⁺, Fe²⁺, Ni²⁺, and Zn²⁺ ions formed with the ligand picolinaldehyde-2-pyridylhydrazone (PapyH) using the Benesi-Hildebrand method. Stoichiometry 2:1 (ligand: metal) was previously determined by the Job’s method and confirmed by single-crystal x-ray diffraction finding a propeller-like structure of the [Fe(Papy)₂] compound PapyH and the metal complexes were characterized by ¹H NMR and UV-visible spectroscopy, resp. The Cu²⁺ complex exhibited the highest stability constant, which was confirmed by competitive reaction of different metal ions with the ligand PapyH.

Inorganica Chimica Acta published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, Name: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine.

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

Wood, Aaron published the artcileCoordinated Hydrazone Ligands as Nucleophiles: Reactions of Fe(papy)₂, Recommanded Product: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, the publication is Inorganic Chemistry (2004), 43(26), 8355-8360, database is CAplus and MEDLINE.

The diamagnetic Fe(II) complexes of the hydrazone ligand pyridinecarboxaldehyde-2′-pyridylhydrazone (papyH) were characterized by NMR, IR, UV-visible, and electrochem. The dication Fe(papyH)₂²⁺ undergoes reversible 1-electron oxidation at 0.66 V vs. internal ferrocene and shows a strong metal-ligand charge-transfer band in the visible region at 524 nm. Deprotonation with NaOH gives diamagnetic, neutral Fe(papy)₂ with an oxidation potential of -0.25 V vs. internal ferrocene and a charge-transfer band at 603 nm. Fe(papy)₂ reacts with active alkylating agents to give dialkyl complexes Fe(papyR)₂²⁺ with spectroscopic properties similar to those of Fe(papyH)₂²⁺. Monitoring the alkylation by UV-visible reveals the intermediacy of a monoalkylated species.

Inorganic Chemistry published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C10H14O, Recommanded Product: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine.

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

Chatterjee, Nachiketa published the artcileA Metal and Base-Free Chemoselective Primary Amination of Boronic Acids Using Cyanamidyl/Arylcyanamidyl Radical as Aminating Species: Synthesis and Mechanistic Studies by Density Functional Theory, Recommanded Product: 2-Pyridinylboronic acid, the publication is Journal of Organic Chemistry (2016), 81(12), 5120-5127, database is CAplus and MEDLINE.

An efficient, metal and base-free, chemoselective synthesis of aryl-, heteroaryl-, and alkyl primary amines from the corresponding boronic acids has been achieved at ambient temperature mediated by [bis(trifluoroacetoxy)iodo]benzene (PIFA) and N-bromosuccinimide (NBS) using cyanamidyl/arylcyanamidyl radicals as the aminating species. The primary amine compounds were initially obtained as their corresponding ammonium trifluoroacetate salts which, on treatment with aq NaOH, provide the free amines. Finally, the primary amines were isolated through column chromatog. over silica-gel using hexane-EtOAc solvent system as the eluent. The reactions are sufficiently fast, completing within 1 h. Quantum chem. calculations in combination with exptl. observations validate that the ipso amination of substituted boronic acids involves the formation of cyanamidyl/arylcyanamidyl radical, followed by regiospecific interaction of its nitrile-N center with boron atom of the boronic acids, leading to chemoselective primary amination.

Journal of Organic Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

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