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Merck Sharp & Dohme Corp.; BRESLIN, Michael J.; COX, Christopher D.; HARTINGH, Timothy J.; PERO, Joseph; RAHEEM, Izzat T.; ROSSI, Michael; VASSALLO, Laura

no abstract published

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1,463-Naphthyridine – Wikipedia,
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Introduction: Central Nervous System (CNS) disorders are on increase perhaps due to genetic, enviromental, social and dietetic factors. Unfortunately, a large number of CNS drugs have adverse effects such as addiction, tolerance, psychological and physical dependence. In view of this, literature search was carried out with a view to identify functional chemical groups that may serve as lead molecules for synthesis of compounds that may have CNS activity. Methods: The search revealed that heterocycles that have heteroatoms such as nitrogen (N), sulphur (S) and oxygen (O) form the largest class of organic compounds. They replace carbon in a benzene ring to form pyridine. Compounds with furan, thiophene, pyrrole, pyridine, azole, imidazole, indole, purine, pyrimidine, esters, carboxylic acid, aldehyde, pyrylium, pyrone, pyrodine, barbituric acid, barbiturate, quinoline, quinolone, isoquinolone, coumarin, alkylpyridine, picoline, piperidine, diazine, carboxamide, flavonoid glycoside, oxindole, aminophenol, benzimidazole, benzoxazole, benzothiazole, and chromone chemical groups among others may have CNS effects ranging from depression passing through euphoria to convulsion. Results and Conclusion: Examples of the compounds with the functional groups include but not limited to coal tar, pyridostigmine, pralidoxime, quinine, mefloquine, pyrilamine, pyronaridine, ciprofloxacin and piroxicam. A number of them can undergo keto-enol tautomerism. Chiral amines may be used for derivation of chiral carboxylic acids which are components of tautomers. Some tautomers may cause parkinsonism and Stevens Johnson syndrome.

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1,244-Naphthyridine – Wikipedia,
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It is well-recognized that N-heterocyclic carbene (NHC) ligands have provided a new dimension to the design of homogeneous catalysts. Part of the success of this type of ligands resides in the limitless access to a variety of topologies with tuned electronic properties, but also in the ability of a family of NHCs that are able to adapt their properties to the specific requirements of individual catalytic transformations. The term “smart” is used here to refer to switchable, multifunctional, adaptable, or tunable ligands and, in general, to all those ligands that are able to modify their steric or electronic properties to fulfill the requirements of a defined catalytic reaction. The purpose of this review is to comprehensively describe all types of smart NHC ligands by focusing attention on the catalytically relevant ligand-based reactivity.

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1,222-Naphthyridine – Wikipedia,
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The 1,8-naphthyridine derivatives have gained special attention from researchers nowadays on account of their demonstrating a variety of interesting biological activities. A wide range of biological activities establishes them as potent scaffolds in therapeutic and medicinal research. The broad spectrum of activities primarily includes antimicrobial, antiviral, anti-inflammatory, anticancer, antihypertensive and analgesic activities. 1,8-Naphthyridine derivatives have also exhibited potential applications in neurological disorders such as Alzheimer?s disease and depression. In addition, these synthetic derivatives have been found to possess activities such as anti-HIV, anti-osteoporotic, alphavbeta3 antagonism, anti-allergic, antimalarial, gastric antisecretory, anticonvulsant, platelet aggregation inhibition, anti-oxidant, Epidermal Growth Factor Receptor (EGFR) inhibition, protein kinase inhibition, ionotropic properties, beta3 antagonism, phosphodiesterase 4 (PDE 4) inhibition, adenosine receptor agonist, adrenoceptors antagonism and DNA stabilizing properties. In this review, we present an update of different 1,8-naphthyridine derivatives and discuss the key data available in the context of various biological activities of 1,8-naphthyridine derivatives available from the literature. This may direct future researches in the synthesis of new derivatives of it and exploring this scaffold for modification of existing biological actions as well as evaluation of other possible pharmacological activities.

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1,128-Naphthyridine – Wikipedia,
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Luminescent materials simultaneously exhibiting superior luminescence efficiency, thermally activated delayed fluorescence (TADF) and aggregation-induced emission (AIE) properties in the solid state are eagerly required for highly efficient non-doped organic light-emitting diodes (OLEDs). Herein, two new emitters, namely ND-AC and CND-AC, featuring a naphthyridine or cyano-naphthyridine segment as the electron acceptor and an acridine unit as the electron donor were designed, synthesized and investigated. The nearly orthogonal molecular configuration of the target emitters not only endows them with small energy differences between singlet and triplet states for ensuring TADF character but also affords a remarkable AIE feature. Due to the high photoluminescence quantum yields, and excellent TADF and AIE characteristics, the doped and non-doped OLEDs based on ND-AC exhibit outstanding performances with maximum external quantum efficiencies of 16.8% and 12.0%, respectively. These results demonstrate that the naphthyridine-based emitters have a promising application in OLEDs.

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Photocatalytic depolymerization (PCDP) of rice husk (RH) over TiO 2 in H2O2 aqueous solution under ultraviolet irradiation was investigated. The reaction mixture was fractionated into different extracts by filtration and subsequent sequential extraction with different organic solvents. In total, 172 organic compounds were identified in the extracts with GC/MS. The compounds can be classified into alkanes, alkenes, arenes, non-substituted alkanols, substituted alkanols, alkenols, phenols, alkanals, alkenals, benzaldehydes, ketones, carboxylic acids, alkanoates, phthalates, nitrogen-containing organic compounds, sulfur-containing organic compounds and other species. Alkanes are the most abundant in the group components. They resulted from the degradation of waxes in RH. Aldehydes and ketones were also detected with high relative contents, most of which were derived from cellulose, hemicellulose and waxes. Phthalates and arenes resulted from lignin degradation. Lignin-wax and hemicellulose-wax interlinkages are proposed to be new structures. According to the species identified in the extracts, the mechanisms for photocatalytic oxidation of benzene ring-containing compounds are proposed. The PCDP of RH provides an alternative way to obtain value-added chemicals from biomass with low energy consumption and under eco-friendly conditions.

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1,183-Naphthyridine – Wikipedia,
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The reactions and synthesis of pyrroles, indoles, isatins, carbazoles and related fused heterocyclic ring systems from the year 2017 are reviewed. Pyrroles and indoles are treated in separate sections with the ring-forming reactions discussed by intramolecular or intermolecular bond disconnection. Other sections include nucleophilic, electrophilic or radical reactivity of the parent rings, C?H functionalization/organometallic reactions, reactions of side chains and examples in total synthesis.

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A new magnetic resonance imaging probe(Gd-NAPTA) with 2-amino-7-methyl-1, 8-naphthyridine as the nucleotide triggering site incorporating into gadolinium-based contrast agent through 2,6-dimethylpyridine linker, preferentially responding to guanosine 5?-triphosphate and adenine 5?-triphosphate has been developed. The formation of strong multi-hydrogen bonds between naphthyridine and nucleotide bases made the phosphate in guanosine 5?-triphosphate and adenine 5?-triphosphate positioned on a suitable site to coordinate to the lanthanide ion, such the substitute of the coordinated pyridine promotes the water molecule close to Gd center and the relaxivity increase of the contrast agent. The longitudinal relaxivity(r1) of Gd-NAPTA could linearly respond to the concentration of guanosine 5?-triphosphate and adenine 5?- triphosphate. The limit of detection (LOD) is about 0.03 mM. The negligible cytotoxicity and appropriate blood circulation time of Gd-NAPTA allow potential application of Magnetic Resonance Imaging in vivo.

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1,164-Naphthyridine – Wikipedia,
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Some scientific research about 7-Chloro-1,8-naphthyridin-2-ol

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WARNER-LAMBERT COMPANY LLC

Compounds of formula (I) are disclosed. A of formula 1 is-(CH2 )mCO-or-(CH2)mCOH-, wherein m is an integer from 2 to 5 and wherein one or two of the carbon atoms can be substituted as described in the specification. G, D, Z, Q, X, Y, R 1, and R4 through R7 of formula 1 are defined in the specification. Also provided are descriptions of processes for preparing compounds of formula 1, intermediates used in making the same, and pharmaceutical compositions containing such compounds and their use in the treatment of central nervous system disorders and other disorders.

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Lithium indenide (Li-Ind) or cyclopentadienide (Li-Cp) derivatives react as nucleophiles with 8-(methylsulfinyl)- 1,5-naphthyridine (Naph), leading to donor-functionalized ligands IndNaph or CpNaph, respectively. The new ligands comprise two N-donor atoms, which, for geometric reasons, cannot bind to the same metal atom. In complexes, where the metal atom is bound by the Cp or Ind moiety, the N5-donor atom is located in a distal position. The coordination behavior to Rh or Zr metal centers has been investigated. The Cp-based ligands show the expected chelating coordination mode with nu5-Cp and N coordination, whereas the indenyl units act as dihapto, trihapto, or pentahapto ligands. The dinuclear Rh(I) complex 12 shows a rare coordination geometry with two nu3 ligands bridging a Rh 2(CO)3 fragment.

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1,402-Naphthyridine – Wikipedia,
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