Pyridine-derivatives

Hameed P., Shahul published the artcileTriaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate, Product Details of C6H8N2, the publication is Nature Communications (2015), 6715, database is CAplus and MEDLINE.

The widespread emergence of Plasmodium falciparum (Pf) strains resistant to frontline agents has fuelled the search for fast-acting agents with novel mechanism of action. Here, we report the discovery and optimization of novel antimalarial compounds, the triaminopyrimidines (TAPs), which emerged from a phenotypic screen against the blood stages of Pf. The clin. candidate (compound 12) is efficacious in a mouse model of Pf malaria with an ED₉₉ <30 mg kg^-1 and displays good in vivo safety margins in guinea pigs and rats. With a predicted half-life of 36 h in humans, a single dose of 260 mg might be sufficient to maintain therapeutic blood concentration for 4-5 days. Whole-genome sequencing of resistant mutants implicates the vacuolar ATP synthase as a genetic determinant of resistance to TAPs. Our studies highlight the potential of TAPs for single-dose treatment of Pf malaria in combination with other agents in clin. development.

Nature Communications published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Product Details of C6H8N2.

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

Qian, Yingjie published the artcileSynthesis of novel and room temperature-operable palladium complexes on graphene oxide: An efficient recyclable catalyst for Suzuki-Miyaura coupling reactions, Application of 2-Bromopyridin-3-amine, the publication is Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) (2019), 253-261, database is CAplus.

Novel palladium complexes composed of palladium and a conjugated ligand (imine-aldehyde) were immobilized on graphene oxide. The developed catalyst was characterized by XPS, and TEM. The novel catalyst was proven to be highly efficient for the Suzuki-Miyaura coupling reaction of aryl halides (Br, Cl) with arylboronic acids under mild conditions with a low amount of catalyst (0.1 mol%). In particular, excellent yields could be also obtained at room temperature within 1 h for monosubstituted aryl bromide coupling. Furthermore, the novel catalyst could be reused at least ten times without significant loss of its catalytic activities.

Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) 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, Application of 2-Bromopyridin-3-amine.

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

Ryan, D. E. published the artcileLigand structure and fluorescence of metal chelates. N-Heterocyclic hydrazones with zinc, Quality Control of 2215-33-0, the publication is Analytica Chimica Acta (1972), 58(1), 101-6, database is CAplus.

-Benzimidazolecarboxaldehyde 2-quinolylhydrazone (I) is the most sensitive reagent of 15 N-containing heterocyclic hydrazones for the fluorimetric determination of Zn; <1 ppb Zn can be determined with excitation and emission wavelengths of 470 and 520

Analytica 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, Quality Control of 2215-33-0.

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

Raftery, Declan P. published the artcileIdentification of hydrogen peroxide as the autoxidation product of N-phenyl-2-propyl-3,5-diethyl-1,2-dihydropyridine, Name: 3,5-Diethyl-1-phenyl-2-propyl-1,2-dihydropyridine, the publication is Analytical Communications (1996), 33(10), 375-379, database is CAplus.

Recently, dihydropyridines were used as autoxidizable materials in novel air-activated adhesives. The dihydropyridines react with air to produce peroxide species, which are capable of initiating free radical polymerization of methacrylates. Probably N-phenyl-2-propyl-3,5-diethyl-1,2-dihydropyridine undergoes autoxidation in the presence of glacial acetic acid, yielding a pyridinium ion and an unknown peroxide product. Employing a variety of anal. techniques, including polarog., spectrophotometry and an enzyme-based biosensor, it was shown conclusively that hydrogen peroxide is generated in the autoxidation of this dihydropyridine. An aqueous extraction procedure was used to remove the hydrogen peroxide from an organic matrix and also to eliminate any interference from the dihydropyridine in the anal. procedure.

Analytical Communications published new progress about 34562-31-7. 34562-31-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 3,5-Diethyl-1-phenyl-2-propyl-1,2-dihydropyridine, and the molecular formula is C18H25N, Name: 3,5-Diethyl-1-phenyl-2-propyl-1,2-dihydropyridine.

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

Roppe, Jeffrey published the artcileDiscovery of Novel Heteroarylazoles That Are Metabotropic Glutamate Subtype 5 Receptor Antagonists with Anxiolytic Activity, Product Details of C6H5F4NO3S, the publication is Journal of Medicinal Chemistry (2004), 47(19), 4645-4648, database is CAplus and MEDLINE.

The highly potent, selective, and brain-penetrant metabotropic glutamate subtype 5 (mGlu5) receptor antagonists 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile and 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile are reported. Compound 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile is active in the rat fear-potentiated startle (FPS) model of anxiety with ED₅₀ = 5.4 mg/kg (po) when dosed acutely. In this model the anxiolytic effects of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile rapidly tolerate on repeated dosing.

Journal of Medicinal Chemistry 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, Product Details of C6H5F4NO3S.

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

Reuss, Robert H. published the artcileCyano adducts of 1-substituted pyridinium salts, Recommanded Product: 1-(Cyanomethyl)pyridin-1-ium chloride, the publication is Journal of Organic Chemistry (1974), 39(14), 2027-31, database is CAplus.

The preparation and characterization of 10 cyano adducts I (R = 4-pyridyl, CH2OMe, Ph, etc.) from 1-substituted pyridinium salts II (X = Cl, Br) is described. In addition, the first Reissert-like compound (III) from pyridine is reported. I are relatively stable.

Journal of Organic Chemistry published new progress about 17281-59-3. 17281-59-3 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitrile,Salt, name is 1-(Cyanomethyl)pyridin-1-ium chloride, and the molecular formula is C7H7ClN2, Recommanded Product: 1-(Cyanomethyl)pyridin-1-ium chloride.

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

Montgomery, Justin I. published the artcileDiscovery and characterization of a novel class of pyrazolopyrimidinedione tRNA synthesis inhibitors, Name: 3-Methoxypyridine-4-boronic acid, the publication is Journal of Antibiotics (2015), 68(6), 361-367, database is CAplus and MEDLINE.

A high-throughput phenotypic screen for novel antibacterial agents led to the discovery of a novel pyrazolopyrimidinedione, PPD-1, with preferential activity against methicillin-resistant Staphylococcus aureus (MRSA). Resistance mapping revealed the likely target of inhibition to be lysyl tRNA synthetase (LysRS). Preliminary structure-activity relationship (SAR) studies led to an analog, PPD-2, which gained Gram-neg. antibacterial activity at the expense of MRSA activity and resistance to this compound mapped to prolyl tRNA synthetase (ProRS). These targets of inhibition were confirmed in vitro, with PPD-1 showing IC₅₀s of 21.7 and 35 μM in purified LysRS and ProRS enzyme assays, and PPD-2, 151 and 0.04 μM, resp. The highly attractive chem. properties of these compounds combined with intriguing preliminary SAR suggest that further exploration of this compelling novel series is warranted.

Journal of Antibiotics 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, Name: 3-Methoxypyridine-4-boronic acid.

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

Cumming, Jared N. published the artcileStructure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor, Safety of 2-Pyridinylboronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(7), 2444-2449, database is CAplus and MEDLINE.

From an initial lead 2-imino-1-methyl-4,4-diphenyl-5-imidazolidinone, a structure-based design approach led to identification of the novel, high-affinity iminohydantoin BACE1 inhibitor I that lowers CNS-derived Aβ following oral administration to rats. SAR development in the S3 and F’ subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for I are reported.

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 C5H6BNO2, Safety of 2-Pyridinylboronic acid.

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

Li, Jianqing published the artcileA Practical Synthesis of the TGFβRI Inhibitor N-(4-(3-(6-(Difluoromethyl)pyridin-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl)pyridin-2-yl)acetamide via One-pot Sequential Sonogashira and Cacchi Reactions Catalyzed by Pd(OAc)₂/BINAP, HPLC of Formula: 39856-58-1, the publication is Organic Process Research & Development (2020), 24(3), 454-458, database is CAplus.

N-(4-(3-(6-(Difluoromethyl)pyridin-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl)pyridin-2-yl)acetamide is a potent inhibitor of TGFβRI kinase that provides durable antitumor activity when combined with an anti-PD-1 antibody. In order to conduct a full range of preclin. studies, over 150 g of high quality material were required. The original discovery route through a step-wise, copper-mediated Sonogashira reaction, trifluoroacetamide formation and Cacchi reaction suffered from scale-up issues, mainly associated with tedious chromatog. purification of intermediates. This communication describes a chromatog.-free, one-pot synthesis of tittle compound via sequential Sonogashira and Cacchi reactions promoted by the superior catalyst Pd(OAc)₂/BINAP, which was discovered by catalyst screening.

Organic Process Research & Development 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, HPLC of Formula: 39856-58-1.

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

Van Beek, Wim E. published the artcileSynthesis of 3,3-Dichloropiperidines and Further Functionalization via Pd-Catalyzed Cross-Coupling Reactions of the Dichloromethylene Moiety, COA of Formula: C5H6BNO2, the publication is European Journal of Organic Chemistry (2019), 2019(1), 95-103, database is CAplus.

A new synthetic methodol. for the functionalization of the dichloromethylene moiety in 3,3-dichloropiperidines via Pd-catalyzed cross-coupling reactions is reported. A range of 3,3-dichloropiperidines was synthesized via a hydride induced cyclization of α,α,δ-trichloroaldimines or an indium(III) triflate catalyzed alkynylation/cyclization procedure of α,α,δ-trichloroaldimines. Subsequently, a dehydrochlorination followed by a cross-coupling with the thus formed vinylic chloride was envisioned. The non-alkynylated 3,3-dichloropiperidines could be regioselectively eliminated and by careful choice of solvent and base both of the two regioisomeric vinyl chlorides could be exclusively formed. Palladium-catalyzed Suzuki cross-coupling of the thus formed 5-chloro-1,2,3,6-tetrahydropyridines led to C3-substituted 1,2,3,6-tetrahydropyridines, which could be easily reduced to 3-substituted piperidines, generating therapeutic agent (±)-Preclamol for example. The 2-alkynyl-3,3-dichloropiperidines were regioselectively eliminated giving the cyclic enamine, which was subsequently cross-coupled in one-pot. The presence of the alkynyl function, in this case, clearly directs elimination towards enamine structures. Hydrogenation of the resulting, unstable 2-alkynyl-3-substituted-1,2,3,4-tetrahydropyridines, yields stable 2,3-disubstituted piperidines.

European 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 C8H6ClF3, COA of Formula: C5H6BNO2.

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