Month: December 2022

Wang, Liang published the artcileRapid, Sustainable, and Gram-Scale Synthesis of Phenols Catalyzed by a Biodegradable Deep Eutectic Mixture in Water, SDS of cas: 197958-29-5, the publication is Asian Journal of Organic Chemistry (2013), 2(12), 1040-1043, database is CAplus.

Mild, rapid, recyclable, gram-scale synthesis of phenols via oxidative hydroxylation of arylboronic acids catalyzed by a biodegradable deep eutectic mixture in water was reported. A broad substrate compatibility, metal- and additive-free conditions, as well as gram-scale synthesis made this procedure more environmentally benign.

Asian 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 0, SDS of cas: 197958-29-5.

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

Bromidge, Steven M. published the artcileBiarylcarbamoylindolines Are Novel and Selective 5-HT_2C Receptor Inverse Agonists: Identification of 5-Methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant/Anxiolytic Agent, Recommanded Product: 5-Nitro-2-phenylpyridine, the publication is Journal of Medicinal Chemistry (2000), 43(6), 1123-1134, database is CAplus and MEDLINE.

The evolution, synthesis, and biol. activity of a novel series of 5-HT_2C receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT_2C affinity and selectivity over 5-HT_2A receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with addnl. selectivity over the closely related 5-HT_2B receptor. Compounds from this series are inverse agonists at the human cloned 5-HT_2C receptor, completely abolishing basal activity in a functional assay. The new series have reduced P 450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biol. profile, SB-228357 and SB-243213 have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.

Journal of Medicinal 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, Recommanded Product: 5-Nitro-2-phenylpyridine.

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

Yule, Ian A. published the artcilePyridine-3-carboxamide-6-yl-ureas as novel inhibitors of bacterial DNA gyrase: Structure based design, synthesis, SAR and antimicrobial activity, Recommanded Product: 4-Amino-2-picoline, the publication is European Journal of Medicinal Chemistry (2014), 31-38, database is CAplus and MEDLINE.

The development of antibacterial drugs based on novel chemotypes is essential to the future management of serious drug resistant infections. We herein report the design, synthesis and SAR of a novel series of N-ethylurea inhibitors based on a pyridine-3-carboxamide scaffold targeting the ATPase sub-unit of DNA gyrase. Consideration of structural aspects of the GyrB ATPase site has aided the development of this series resulting in derivatives that demonstrate excellent enzyme inhibitory activity coupled to potent Gram pos. antibacterial efficacy.

European Journal of Medicinal Chemistry 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 C6H12N2O, Recommanded Product: 4-Amino-2-picoline.

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

Dunn, A. D. published the artcileBromination of Pyridines. II. Bromination of aminopicolines, Computed Properties of 18437-58-6, the publication is Journal fuer Praktische Chemie (Leipzig) (1989), 331(3), 369-74, database is CAplus.

The bromination of all 10 possible aminopicolines was investigated. In general, the major brominated product was that corresponding to electrophilic attack at the site para or ortho to the amino group.

Journal fuer Praktische Chemie (Leipzig) 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, Computed Properties of 18437-58-6.

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

Kool, Eric T. published the artcileFast Alpha Nucleophiles: Structures that Undergo Rapid Hydrazone/Oxime Formation at Neutral pH, Recommanded Product: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, the publication is Organic Letters (2014), 16(5), 1454-1457, database is CAplus and MEDLINE.

Hydrazones and oximes are widely useful structures for conjugate formation in chem. and biol., but their formation can be slow at neutral pH. Kinetics studies were performed for a range of structurally varied hydrazines, and a surprisingly large variation in reaction rate was observed Structures that undergo especially rapid reactions were identified, enabling reaction rates that rival orthogonal cycloaddition-based conjugation chemistries.

Organic Letters 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, Recommanded Product: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine.

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

Saget, Tanguy published the artcileEnantioselective C-H Arylation Strategy for Functionalized Dibenzazepinones with Quaternary Stereocenters, Recommanded Product: 2-Bromopyridin-3-amine, the publication is Angewandte Chemie, International Edition (2013), 52(30), 7865-7868, database is CAplus and MEDLINE.

Reported here is a new and mild enantioselective palladium(0)-catalyzed direct arylation to access highly functionalized and relevant dibenzazepinones possessing a quaternary stereocenter with excellent selectivities. The enantiodiscriminating CMD step occurs through a rare eight-membered palladacycle, which is unprecedented for an enantioselective process. With these substrates, a complete selectivity over competing C-H activations, which could give five- or six-membered rings, was found. Addnl. noteworthy features of the process are its good functional-group compatibility and the use of cheap and widely available taddol phosphoramidites as chiral ligands.

Angewandte Chemie, International Edition 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

Hucke, Oliver published the artcileMolecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency, Recommanded Product: (6-Amino-5-methylpyridin-3-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2014), 57(5), 1932-1943, database is CAplus and MEDLINE.

The design and preliminary SAR of a new series of 1H-quinazolin-4-one (QAZ) allosteric HCV NS5B thumb pocket 2 (TP-2) inhibitors was recently reported. To support optimization efforts, a mol. dynamics (MD) based modeling work-flow was implemented, providing information on QAZ binding interactions with NS5B. This approach predicted a small but critical ligand-binding induced movement of a protein backbone region which increases the pocket size and improves access to the backbone carbonyl groups of Val 494 and Pro 495. This localized backbone shift was consistent with key SAR results and was subsequently confirmed by X-ray crystallog. The MD protocol guided the design of inhibitors, exploiting novel H-bond interactions with the two backbone carbonyl groups, leading to the first thumb pocket 2 NS5B inhibitor with picomolar antiviral potency in genotype (gt) 1a and 1b replicons (EC₅₀ = 120 and 110 pM, resp.) and with EC₅₀ ≤ 80 nM against gt 2-6.

Journal of Medicinal Chemistry published new progress about 1032759-01-5. 1032759-01-5 belongs to pyridine-derivatives, auxiliary class Boronic acid and ester,Boronic acid and ester, name is (6-Amino-5-methylpyridin-3-yl)boronic acid, and the molecular formula is C6H9BN2O2, Recommanded Product: (6-Amino-5-methylpyridin-3-yl)boronic acid.

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

Proenca, M. Fernanda published the artcileOne-pot approach to the synthesis of novel 12H-chromeno[2′,3′:4,5]imidazo[1,2-a]pyridines in aqueous media, HPLC of Formula: 17281-59-3, the publication is Tetrahedron (2010), 66(25), 4542-4550, database is CAplus.

The chromeno-imidazo[1,2-a]pyridine scaffold was generated in a one pot condensation/cyclization reaction involving a salicylaldehyde and 1-(cyanomethyl)pyridinium chloride in aqueous sodium carbonate solution These novel compounds, e.g., I, were isolated in 47-71% yield. The reaction pathway was followed by ¹H NMR spectroscopy allowing a clear understanding of the side reactions involved in the process. Different mono-substituted pyridinium chlorides were synthesized and reacted with mono-substituted salicylaldehydes and a detailed discussion of the scope of the synthetic method is also presented.

Tetrahedron 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

Proenca, Fernanda published the artcileA one-pot synthesis of substituted pyrido[2,3-b]indolizines, HPLC of Formula: 17281-59-3, the publication is Tetrahedron (2011), 67(6), 1071-1075, database is CAplus.

An efficient and novel approach to the synthesis of substituted pyrido[2,3-b]indolizine-10-carbonitriles (I; R¹, R² = Me, aryl) was developed. These structures are practically unavailable through previously described methods. The cascade transformation involves the reaction of α,β-unsaturated carbonyl compounds with a stable dimer prepared from 1-(cyanomethyl)pyridinium chloride. The reaction was performed under reflux conditions in ethanol/water and in the presence of sodium acetate. This procedure represents a eco-friendly regioselective approach to the pyrido[2,3-b]indolizine core structure.

Tetrahedron 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

Lima, Cristovao F. published the artcileNovel structurally similar chromene derivatives with opposing effects on p53 and apoptosis mechanisms in colorectal HCT116 cancer cells, COA of Formula: C7H7ClN2, the publication is European Journal of Pharmaceutical Sciences (2015), 34-45, database is CAplus and MEDLINE.

In the present work, novel chromene derivatives fused with the imidazo[1,2-a]pyridine nucleus were tested for their anticancer potential in the human colorectal cancer HCT116 cells. Compounds 2a and 2c showed significant growth inhibitory activity with GI50 of 15 μM and 11 μM, resp. Compound 2c, the most potent, has a carbamate group in position 8 of the pyridine ring, and showed significant cell cycle arrest and induction of cell death by apoptosis, even at 5 μM. Besides different potencies, chromene analogs 2a and 2c showed different mechanisms of action. Whereas the carbamate-free chromene 2a induced cell cycle arrest at G1/G0 phase, compound 2c showed to arrest cell cycle at both S and G2 phases. Chromene derivative 2a at concentrations higher than its GI50 remarkably induced caspases-dependent apoptosis in a p53-independent manner. On the other hand, compound 2c increased significantly p53 levels and induced apoptosis in a p53- and caspases-dependent manner, even at concentrations lower than its GI50. Both compounds increased the Bax/Bcl-2 ratio, induced mitochondria depolarization and activated MAP kinases. In conclusion, two novel and structurally similar chromene derivatives showed cytotoxicity to HCT16 cells through opposing effects on p53 levels and apoptosis mechanisms, which may be relevant for further development of drugs acting on distinct mol. targets useful in the treatment of cancers with different genetic profiles and for personalized medicine.

European Journal of Pharmaceutical Sciences 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, COA of Formula: C7H7ClN2.

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