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The tachykinin NK2 receptor is widel y distributed in the peripheral and central nervou s system. It mediates numerous pharmacologi cal effects of neurokinin A, suggesting that the tachykinin NK2 receptor may be possible target for new therapeutics. Many effor ts to identify and cha racterize selective antagonists of thi s receptor have been undertaken and several antagonists of both peptide and nonpeptide nature have been disclosed. Among th ese compounds, nepadutant, a peptide-based antagonist, and saredutant, a nonpeptide antagoni st, are certainly among the most potent compounds. These two antagonists combine high affinity for the human tachykinin NK2 receptor with strong antagonist activities in a large variety of in vitro and in vivo pharmacological models. Contrary to nepadutant, saredutant has been shown to be orally active. In addition to th eir potent acti vitie s in the airways they show potent inhibitory activities in visceral nociception suggesting that a tach ykinin NK2 receptor antagonist may be useful for the tre atment of functional gastrointestinal disorders such as irritable bowel syndrome. With the use of saredutant, major progress has also been made in the understanding of the role of brain tachykinin NK2 receptors. Contrary to nepadutant, saredutant is centrally active and shows antidepressant/anxiolytic activity.

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Reference£º
1,110-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N104 – PubChem

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Reference of 100361-18-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.100361-18-0, Name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid, molecular formula is C12H8ClFN2O3. In a Patent£¬once mentioned of 100361-18-0

Warner-Lambert Company

Novel, orally active antibacterial agents are described and characterized as 7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acids or corresponding 1,8-naphthyridine derivatives as well as methods for their manufacture.

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Reference£º
1,666-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N660 – PubChem

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PEGylated chitosan-based nanoparticles offer attractive platforms for siRNA cocktail delivery into tumors. Still, therapeutic efficacy requires us to select a rational combination of siRNAs and an efficient tumor delivery after systemic administration. Here, we showed that non-covalent PEGylation of chitosan-based nanoparticles loaded with siRNA targeting two key transporters of energy fuels for cancer cells, namely the lactate transporter MCT1 and the glutamine transporter ASCT2, could lead to significant antitumor effects. As a ligand, we tested variations of the prototypical RGD peptidomimetic (RGDp). A higher siRNA delivery was obtained with naphthyridine-containing RGDp randomly conjugated on the PEG chain by clip photochemistry and the use of a lipophilic linker than when using traditional chain-end grafting and RGDp with a hydrophilic linker. The antiproliferative effects resulting from ASCT2 and MCT1 silencing were validated separately in vitro in conditions mimicking specific metabolic profiles of cancer cells and in vivo upon concomitant delivery. The combination of those siRNA and the selected components of targeted RGDp nanoparticles led to a dramatic tumor growth inhibition upon peri-tumoral but also systemic administration in mice. Altogether these data emphasize the convenience of using non-covalent PEGylated chitosan particles to produce sheddable stealth protection compatible with an efficient siRNA delivery in tumors.

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Reference£º
1,91-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N85 – PubChem

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A pyrene-based colorimetric and fluorescent pH probe with large Stokes shift (145 nm) was developed. PNY afforded a pKa of 2.98 and responded linearly to minor pH changes within the range of 2.43 and 3.71. In addition, PNY could be used for detecting H+ with high sensitivity and selectivity, showing colorimetric and fluorometric dual-modal responses with short response time. Furthermore, PNY had good photostability, excellent reversibility and cell membrane permeability. Significantly, PNY could image acidic pH in A549 cells and visualized extreme acidity in E. coli cells.

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Reference£º
1,84-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N78 – PubChem

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Laboratoire Roger Bellon

New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R1 is a hydrogen atom or a hydroxyl or alkyl radical, R2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkyloxy or alkylamino radical, R3 is a phenyl or phenylalkyl radical substituted with one or more halogen atoms or alkyl, cycloalkyl (3 to 6 C), alkyloxy, cyano, amino, alkylamino, dialkylamino, alkyloxyalkyl, hydroxyalkyl, hydroxyalkyloxy, methylenedioxy, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl radicals, or R3 is a heterocyclic radical, and R4 is a hydrogen atom or a fluorine atom, the alkyl radicals (1 to 4 C) being linear or branched, their salts, their preparation and compositions containing them. These new products are useful as antimicrobials, or in the treatment of AIDS. STR1

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1,18-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N12 – PubChem

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Related Products of 16287-97-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.16287-97-1, Name is 4-Chloro-1,7-naphthyridine, molecular formula is C8H5ClN2. In a article£¬once mentioned of 16287-97-1

MERCK SHARP & DOHME CORP.; COBURN, Craig, A.; MALETIC, Milana, M.; LUO, Yunfu; QI, Zhiqi; LI, Chun Sing; YU, Tingting

The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

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1,496-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N490 – PubChem

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Glycosylation of 3-alkyl N4-(3-hydroxypropyl) 2-piperazinones by ptotected 1-O-acetyl ribofuranoses produces nucleoside analogs in which the base is separated from the sugar by a hydrocarbon spacer arm.The preliminary in vitro test results against retroviruses seem promising for compounds bearing a long alkyl chain.

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1,435-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N429 – PubChem

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Reference of 254-60-4, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.254-60-4, Name is 1,8-Diazanaphthalene, molecular formula is C8H6N2. In a article£¬once mentioned of 254-60-4

The reaction of indole (2-methylindole) with 1,5-, 1,6-, and 1,8-naphthyridines at 20 deg C, in the presence of benzoyl chloride, leads to the preferential formation of dihydro structures with one indolyl substituent at the alpha-position to the hetero atom.With increase in temperature, dibenzoyl and monobenzoyl tetrahydro-substituted naphthyridines with two indolyl residues in both pyridine ring are formed besides the above compounds.

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1,253-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N247 – PubChem

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Due to the difficulty in achieving high efficiency and high color purity simultaneously, blue emission is the limiting factor for the performance and stability of OLEDs. Since 2003, we have been working on organic light-emitting diodes (OLEDs), especially on blue light. After a series of molecular designs, novel strategies have been proposed from different aspects. At first, highly efficient deep blue emission could be achieved through molecular design with highly twisted structure to suppress fluorescence quenching and redshift. Deep blue emitters with high efficiency in solid state, a twisted structure with aggregation induced emission (AIE) characteristics was incorporated to inhibit molecular aggregation, and triplet-triplet fusion (TTF) and hybridized localized charge transfer (HLCT) were adopted to increase the ratio of triplet exciton used. Secondly, a highly efficient blue OLED could be achieved through improving charge transport. New electron transport materials (ETMs) with wide band gap were developed to control charge transport balance in devices. Thirdly, a highly efficient deep blue emission could be achieved through a mesoscopic structure of out-coupling layer. A mesoscopic photonic structured organic thin film was fabricated on the top of metal electrode by self-aggregation in order to improve the light out-coupling efficiency.

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1,65-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N59 – PubChem

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Because of the peculiar dynamic covalent reactivity of boronic acids to form tetraboronate derivatives, interest in using their aryl derivatives in materials science and supramolecular chemistry has risen. Nevertheless, their ability to form H-bonded complexes has been only marginally touched. Herein we report the first solution and solid-state binding studies of the first double-H-bonded DD¡¤AA-type complexes of a series of aromatic boronic acids that adopt a syn-syn conformation with suitable complementary H-bonding acceptor partners. The first determination of the association constant (Ka) of ortho-substituted boronic acids in solution showed that Ka for 1:1 association is in the range between 300 and 6900 M-1. Crystallization of dimeric 1:1 and trimeric 1:2 and 2:1 complexes enabled an in-depth examination of these complexes in the solid state, proving the selection of the -B(OH)2 syn-syn conformer through a pair of frontal H-bonds with the relevant AA partner. Non-ortho-substituted boronic acids result in “flat” complexes. On the other hand, sterically demanding analogues bearing ortho substituents strive to retain their recognition properties by rotation of the ArB(OH)2 moiety, forming “T-shaped” complexes. Solid-state studies of a diboronic acid and a tetraazanaphthacene provided for the first time the formation of a supramolecular H-bonded polymeric ribbon. On the basis of the conformational dynamicity of the -B(OH)2 functional group, it is expected that these findings will also open new possibilities in metal-free catalysis or organic crystal engineering, where double-H-bonding donor boronic acids could act as suitable organocatalysts or templates for the development of functional materials with tailored organizational properties.

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Reference£º
1,117-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N111 – PubChem