Tag: M.W=150-200

Wall, Mark J. published the artcileDiscovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Ca_v 2.2) blockers for the treatment of pain, HPLC of Formula: 612845-44-0, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(23-24), 3780-3783, database is CAplus and MEDLINE.

A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiol. assay. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.

Bioorganic & Medicinal Chemistry Letters published new progress about 612845-44-0. 612845-44-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Boronic Acids,Boronic acid and ester, name is (6-Ethoxypyridin-3-yl)boronic acid, and the molecular formula is C6H16OSi, HPLC of Formula: 612845-44-0.

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

Kakehi, Akikazu published the artcilePreparation of new nitrogen-bridged heterocycles. 60. Syntheses and conformational analyses of bis(indolizin-1-yl) disulfides, HPLC of Formula: 17281-59-3, the publication is Chemical & Pharmaceutical Bulletin (2007), 55(10), 1458-1465, database is CAplus and MEDLINE.

Bis(indolizin-1-yl) disulfides I (R = cyano, CO₂Et, COPh, R¹ = Me, Et, CH₂Ph, etc., R² = H, Me), readily obtainable from the treatment of 1-(benzoylthio)indolizines II with piperidine, were prepared and their conformations were investigated. In comparison with those of 1-(benzoylthio)indolizines, the ¹H-NMR spectra of these disulfides showed considerable high field shifts (δ 0.13-0.82 ppm) on each pyridine ring proton and the UV spectra exhibited significant bathochromic and hyperchromic shifts. These results supported strongly the participation of an intramol. π-π interaction between two indolizine rings in these mols. and, hence, of a particular gauche (cis) conformation. However, the conformational considerations and mol. calculations (Mopac PM3) for some bis(indolizin-1-yl) disulfides showed the presence of four more stable gauche forms in which two are enantiomeric, resulting in three types of gauche structures. These three types of gauche structures were confirmed by X-ray analyses.

Chemical & Pharmaceutical Bulletin 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, HPLC of Formula: 17281-59-3.

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

Kakehi, Akikazu published the artcilePreparation of new nitrogen-bridged heterocycles. 72. A new approach to 1-acyl-3-(substituted methylthio)thieno[3′,4′:4,5]imidazo[1,5-a]pyridine derivatives, HPLC of Formula: 17281-59-3, the publication is Chemical & Pharmaceutical Bulletin (2010), 58(11), 1502-1510, database is CAplus and MEDLINE.

The alk. treatment of the pyridinium salts, readily available from the S-alkylation of 3-amino-4-(1-pyridinio)thiophene-5-thiolates with various alkyl halides, in chloroform at room temperature afforded the corresponding thieno[3′,4′:4,5]imidazo[1,2-a]pyridine derivatives, e.g., I (R = Ph, 4-ClC₆H₄, OEt, etc., R⁴ = H, Me, PhCH₂, Ph, etc.), in low to moderate yields via the intramol. cyclization of the resulting 1,5-dipoles followed by the aromatization of the primary cycloadducts. Interestingly, the reactions using unsym. 3-amino-4-[1-(3-methylpyridinio)]thiophene-5-thiolates afforded only 8-methylthieno[3′,4′:4,5]imidazo[1,2-a]pyridines and the other 6-Me derivatives were not formed at all. In addition, the isolation of a byproduct in the condensation reaction of pyridinium salt with the solvent (CHCl₃) is also discussed.

Chemical & Pharmaceutical Bulletin 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, HPLC of Formula: 17281-59-3.

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

Adamek, Rebecca N. published the artcileHydroxypyridinethione Inhibitors of Human Insulin-Degrading Enzyme, Recommanded Product: 2-Bromopyridin-3-amine, the publication is ChemMedChem (2021), 16(11), 1775-1787, database is CAplus and MEDLINE.

Insulin-degrading enzyme (IDE) is a human mononuclear Zn2+-dependent metalloenzyme that is widely regarded as the primary peptidase responsible for insulin degradation Despite its name, IDE is also critically involved in the hydrolysis of several other disparate peptide hormones, including glucagon, amylin, and the amyloid β-protein. As such, the study of IDE inhibition is highly relevant to deciphering the role of IDE in conditions such as type-2 diabetes mellitus and Alzheimer disease. There have been few reported IDE inhibitors, and of these, inhibitors that directly target the active-site Zn2+ ion have yet to be fully explored. In an effort to discover new, zinc-targeting inhibitors of IDE, a library of âˆ?50 metal-binding pharmacophores was screened against IDE, resulting in the identification of 1-hydroxypyridine-2-thione (1,2-HOPTO) as an effective Zn2+-binding scaffold. Screening a focused library of HOPTO compounds identified 3-sulfonamide derivatives of 1,2-HOPTO as inhibitors of IDE (Ki values of âˆ?0μM). Further structure-activity relationship studies yielded several thiophene-sulfonamide HOPTO derivatives with good, broad-spectrum activity against IDE that have the potential to be useful pharmacol. tools for future studies of IDE.

ChemMedChem 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, Recommanded Product: 2-Bromopyridin-3-amine.

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

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

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

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

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

Sugimura, Yukio published the artcileSeven-membered ring compounds. XXXVIII. Reaction of troponoid with ylide. III. Reaction of tropone with pyridinium compounds, Quality Control of 17281-59-3, the publication is Bulletin of the Chemical Society of Japan (1972), 45(10), 3174-8, database is CAplus.

Phenacylpyridinium ylide (I, R = H, Br) reacted with tropone to afford 2-hydroxy-2-phenyl-3-phenacyl-2H-cyclohepta[b]furan (II) which was converted into 2-(1,2-dibenzoylethyl)tropone. The reactions of tropone with several kinds of pyridinium bromides yielded 2-substituted tropones in the presence of amines and 1-azaazulene derivatives including III in a one-step formation in the presence of NH4OAc.

Bulletin of the Chemical Society of Japan 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 C3H3Br2ClO, Quality Control of 17281-59-3.

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