Month: October 2022

Andaloussi, Mounir; Moreau, Emmanuel; Masurier, Nicolas; Lacroix, Jacques; Gaudreault, Rene C.; Chezal, Jean-Michel; El Laghdach, Anas; Canitrot, Damien; Debiton, Eric; Teulade, Jean-Claude; Chavignon, Olivier published the artcile< Novel imidazo[1,2-a]naphthyridinic systems (Part 1): Synthesis, antiproliferative and DNA-intercalating activities>, Safety of 6-Amino-3-nitro-2-picoline, the main research area is imidazonaphthonaphthyridine preparation antiproliferative DNA intercalation.

Novel imidazo[1,2-a]naphthyridine systems were obtained from Friedlaender’s reaction in imidazo[1,2-a]pyridine series. The compounds were evaluated for their antitumor activity in the NCIs in vitro human tumor cell line screening panel. Among them, 7,8-dihydroimidazo[1,2-a]naphtho[2,1-g][1,5]naphthyridine and 8,9-dihydroimidazo[1,2-h]naphtho[1,2-b][1,7]naphthyridine exhibited in vitro activity comparable to anticancer agent such as amsacrine. Their mechanism of cytotoxic action was unrelated to poisoning or inhibiting abilities against topo1. On the contrary, a direct intercalation of the drugs into DNA was observed by electrophoresis on agarose gel.

European Journal of Medicinal Chemistry published new progress about Cytotoxic agents. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Safety of 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Di Fabio, Romano; Arban, Roberto; Bernasconi, Giovanni; Braggio, Simone; Blaney, Frank E.; Capelli, Anna M.; Castiglioni, Emiliano; Donati, Daniele; Fazzolari, Elettra; Ratti, Emiliangelo; Feriani, Aldo; Contini, Stefania; Gentile, Gabriella; Ghirlanda, Damiano; Sabbatini, Fabio M.; Andreotti, Daniele; Spada, Simone; Marchioro, Carla; Worby, Angela; St-Denis, Yves published the artcile< Dihydropyrrole[2,3-d]pyridine Derivatives as Novel Corticotropin-Releasing Factor-1 Antagonists: Mapping of the Receptor Binding Pocket by in Silico Docking Studies>, COA of Formula: C9H9Cl2NO2, the main research area is pyrrolo pyridine preparation CRF1 antagonist antidepressant SAR.

In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochem. properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent Ph ring and the nature of the heterocyclic moieties present in the upper region of the mol. Selective and potent compounds have been discovered endowed with reduced ClogP with respect to compounds known in the literature. Of particular relevance was the finding that the in vitro affinity of the series was maintained by reducing the overall lipophilicity. The results achieved by this exploration enabled the formulation of a novel hypothesis on the nature of the receptor binding pocket of this class of CRF-1 receptor antagonists, making use of in silico docking studies of the putative nonpeptidic antagonist binding site set up in house by homol. modeling techniques.

Journal of Medicinal Chemistry published new progress about Antidepressants. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, COA of Formula: C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Matsa, Ramkishore; Makam, Parameshwar; Sethi, Guneswar; Thottasseri, Ahammed Ameen; Kizhakkandiyil, Aswani Raj; Ramadas, Krishna; Mariappan, Vignesh; Pillai, Agieshkumar Balakrishna; Kannan, Tharanikkarasu published the artcile< Pyridine appended 2-hydrazinylthiazole derivatives: design, synthesis, in vitro and in silico antimycobacterial studies>, Quality Control of 350-03-8, the main research area is hydrazinyl thiazole pyridinyl preparation docking antitubercular cytotoxicity lipophilicity.

An array of pyridine appended 2-hydrazinylthiazole derivatives I (R1 = Me, Ph, 1-naphthyl, 3-pyridyl, etc.; R2 = H, Me) has been synthesized to discover novel chemotherapeutic agents for Mycobacterium tuberculosis (Mtb). The drug-likeness of pyridine appended 2-hydrazinylthiazole derivatives I was validated using the Lipinski and Veber rules. The designed thiazole mols. have been synthesized through Hantzsch thiazole methodologies. The in vitro antimycobacterial studies have been conducted using Luciferase reporter phage (LRP) assay. Out of thirty derivatives, the compounds I (R1 = Ph, R2 = H, Me; R1 = 2-FC6H4, R2 = H; R1 = 4-FC6H4, R2 = Me) exhibited good antimycobacterial activity against Mtb, an H37Rv strain, with the min. inhibitory concentration in the range of 6.40-7.14μM. In addition, in vitro cytotoxicity of active mols. has been observed against Human Embryonic Kidney Cell lines (HEK293t) using MTT assay. The compounds I (R1 = Ph, 4-FC6H4; R2 = Me) are nontoxic and their cell viability is 87% and 96.71% resp. The in silico analyses of the pyridine appended 2-hydrazinylthiazole derivatives have been used to find the mode of binding of the active compounds with KasA protein of Mtb. The active compounds showed a strong binding score (-5.27 to -6.23 kcal mol-1).

RSC Advances published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Quality Control of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Edelsbacher, Philipp; Redhammer, Guenther; Monkowius, Uwe published the artcile< Copper(II) complexes bearing cyclobutanecarboxylate and pyridine ligands: a new series of dinuclear paddle-wheel complexes>, Related Products of 93-60-7, the main research area is copper cyclobutanecarboxylate pyridine complex preparation; crystal structure copper cyclobutanecarboxylate pyridine.

Four members of a new series of paddle-wheel copper(II) complexes bearing cyclobutanecarboxylate as bridging ligand with pyridine derived ligands in axial positions are reported. They have been characterized by FTIR-ATR, UV-Vis spectroscopy, mass spectrometry, and single crystal X-ray diffraction. The synthesis is straight-forward by combining the carboxylic acid, copper(II) acetate, and a slight excess of a pyridine ligand. The mol. structures of three complexes reveal a coordination mode expected for such type of dinuclear copper(II) carboxylates.

Monatshefte fuer Chemie published new progress about Crystal structure. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Related Products of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dyck, Brian; Grigoriadis, Dimitri E.; Gross, Raymond S.; Guo, Zhiqiang; Marinkovic, Dragan; McCarthy, James R.; Moorjani, Manisha; Regan, Collin F.; Saunders, John; Schwaebe, Michael K.; Szabo, Tomas; Williams, John P.; Zhang, Xiaohu; Bozigian, Haig; Chen, Ta Kung published the artcile< Potent, Orally Active Corticotropin-Releasing Factor Receptor-1 Antagonists Containing a Tricyclic Pyrrolopyridine or Pyrazolopyridine Core>, Application of C9H9Cl2NO2, the main research area is oral CRF1 receptor antagonist tricyclic pyrrolopyridine pyrazolopyridine core preparation.

Two new classes of tricyclic-based corticotropin-releasing factor (CRF1) receptor-1 antagonists were designed by constraining known 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine ligands. Pyrrole- and pyrazole-based mols. 19g and 22a, resp., were discovered that potently bind the recombinant CRF1 receptor (Ki = 3.5, 2.9 nM) and inhibit adrenocorticotropic hormone (ACTH) release from rat pituitary cell culture (IC50 = 14, 6.8 nM). These compounds show good oral bioavailability (F = 24%, 7.0%) and serum half-lives in rats (t1/2 = 6.3, 12 h) and penetrate the rat brain ([brain]/[plasma] = 0.27, 0.52) but tend toward large volumes of distribution (VD = 38, 44 L kg-1) and rapid clearances (CL = 70, 43 mL min-1 kg-1). When given orally, both the pyrazole and the pyrrole leads dose-dependently inhibit stress-induced ACTH release in vivo. ACTH reductions of 84-86% were observed for 30 mg kg-1 doses.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier (penetration). 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Application of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lenstra, Danny C.; Lenting, Peter E.; Mecinovic, Jasmin published the artcile< Sustainable organophosphorus-catalysed Staudinger reduction>, Name: 2-Fluoro-3-(hydroxymethyl)pyridine, the main research area is amine green preparation; azide Staudinger reduction.

A highly efficient and sustainable catalytic Staudinger reduction for the conversion of organic azides to amines in excellent yields was developed. The reaction displayed excellent functional group tolerance to functionalities that were otherwise prone to reduction, such as sulfones, esters, amides, ketones, nitriles, alkenes and benzyl ethers. The green nature of the reaction was exemplified by the use of PMHS, CPME and a lack of column chromatog.

Green Chemistry published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 131747-55-2 belongs to class pyridine-derivatives, and the molecular formula is C6H6FNO, Name: 2-Fluoro-3-(hydroxymethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Qin, Lei; Zhou, Guo-Jun; Yu, You-Zhu; Nojiri, Hiroyuki; Schroder, Christian; Winpenny, Richard E. P.; Zheng, Yan-Zhen published the artcile< Topological Self-Assembly of Highly Symmetric Lanthanide Clusters: A Magnetic Study of Exchange-Coupling ""Fingerprints"" in Giant Gadolinium(III) Cages>, Computed Properties of 73018-09-4, the main research area is gadolinium cage self assembly magnetization exchange interaction crystal structure.

The creation of a perfect hollow nanoscopic sphere of metal centers is clearly an unrealizable synthetic challenge. It is, however, an inspirational challenge from the viewpoint of chem. architecture and also as finite mol. species may provide unique microscopic insight into the origin and onset of phenomena such as topol. spin-frustration effects found in infinite 2D and 3D systems. Herein, we report a series of high-symmetry gadolinium(III) (S = 7/2) polyhedra, Gd20, Gd32, Gd50, and Gd60, to test an approach based on assembling polymetallic fragments that contain different polygons. Structural anal. reveals that the Gd20 cage resembles a dodecahedron; the vertices of the Gd32 polyhedron exactly reveal symmetry Oh; Gd50 displays an unprecedented polyhedron in which an icosidodecahedron Gd30 core is encapsulated by an outer Gd20 dodecahedral shell with approx. Ih symmetry; and the Gd60 shows a truncated octahedron geometry. Exptl. and theor. magnetic studies show that this series produces the expected antiferromagnetic interaction that can be modeled based on classical spins at the Gd sites. From the magnetization analyses, we can roughly correlate the derivative bands to the Gd-O-Gd angles. Such a magneto-structural correlation may be used as “”fingerprints”” to identify these cages.

Journal of the American Chemical Society published new progress about Antiferromagnetic exchange. 73018-09-4 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Computed Properties of 73018-09-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Babaev, Eugene V.; Rybakov, Victor B. published the artcile< Phenacylation of 6-methyl-beta-nitropyridin-2-ones and further heterocyclization of products>, Product Details of C6H7N3O2, the main research area is betanitropyridinone phenacylation; phenacylpyridone heterocyclization; 8-nitro-5-RO-indolizines; Phenacylation of beta-nitropyridin-2-ones; oxazole-pyrrole ring transformation.

Reaction between the derivatives of 6-methyl-beta-nitropyridin-2-one and phenacyl bromides was studied, and the yields observed were extremely low. The pyridones were converted via chloropyridines to methoxyderivatives, which were N-phenacylated. N-Phenacyl derivatives of 4,6-dimethyl-5-nitropyridin-2-one under the action of base gave 5-hydroxy-8-nitroindolizine and under acidic conditions gave 5-methyl-6-nitrooxazole[3,2-a]pyridinium salt, which underwent recyclization with MeONa to 5-methoxy-8-nitroindolizine.

Molecules published new progress about Acylation. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Product Details of C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Niroobakhsh, Zahra; LaNasa, Jacob A.; Belmonte, Andrew; Hickey, Robert J. published the artcile< Rapid Stabilization of Immiscible Fluids using Nanostructured Interfaces via Surfactant Association>, Safety of 1-Hexadecylpyridin-1-ium chloride, the main research area is nanostructured interface immiscible fluid rapid stabilization.

Surfactant mols. have been extensively used as emulsifying agents to stabilize immiscible fluids. Droplet stability has been shown to be increased when ordered nanoscale phases form at the interface of the two fluids due to surfactant association Here, we report on using mixtures of a cationic surfactant and long chained alkenes with polar head groups [e.g., cetylpyridinium chloride (CPCl) and oleic acid] to create an ordered nanoscale lamellar morphol. at aqueous-oil interfaces. The self-assembled nanostructure at the liquid-liquid interface was characterized using small-angle x-ray scattering, and the mech. properties were measured using interfacial rheol. We hypothesize that the resulting lamellar morphol. at the liquid-liquid interface is driven by the change in critical packing parameter when the CPCl mols. are diluted by the presence of the long chain alkenes with polar head groups, which leads to a spherical micelle-to-lamellar phase transition. The work presented here has larger implications for using nanostructured interfacial material to sep. different fluids in flowing conditions for biosystems and in 3D printing technol.

Physical Review Letters published new progress about Encapsulation Role: PEP (Physical, Engineering or Chemical Process), PROC (Process). 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Safety of 1-Hexadecylpyridin-1-ium chloride.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhao, Changgui; Ye, Zhengqing; Ma, Zhi-xiong; Wildman, Scott A.; Blaszczyk, Stephanie A.; Hu, Lihong; Guizei, Ilia A.; Tang, Weiping published the artcile< A general strategy for diversifying complex natural products to polycyclic scaffolds with medium-sized rings>, HPLC of Formula: 3731-53-1, the main research area is polycyclic steroid preparation oxidation ring expastion natural product.

The interrogation of complex biol. pathways demands diverse small mol. tool compounds, which can often lead to important therapeutics for the treatment of human diseases. Since natural products are the most valuable source for the discovery of therapeutics, the derivatization of natural products has been extensively investigated to generate mols. for biol. screenings. However, most previous approaches only modified a limited number of functional groups, which resulted in a limited number of skeleta. Here, a general strategy for the preparation of a library of complex small mols. by combining state-of-the-art chem. – the site-selective oxidation of C-H bonds – with reactions that expand rigid, small rings in polycyclic steroids to medium-sized rings is described. This library occupies a unique chem. space compared to selected diverse reference compounds The diversification strategy developed herein for steroids can also be expanded to other types of natural products.

Nature Communications published new progress about Alkylation. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, HPLC of Formula: 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem