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FUJIFILM Corporation; FURUYAMA, Hidetomo; KURIHARA, Hideki; TERAO, Takahiro; NAKAGAWA, Daisuke; TANABE, Shintaro; KATO, Takayuki; YAMAMOTO, Masahiko; SEKINE, Shinichiro; MASHIKO, Tomoyuki; INUKI, Shinsuke; UEDA, Satoshi

A compound represented by Formula [1] (in the formula, Z1 represents N, CH, or the like; X1 represents NH or the like; R1 represents a heteroaryl group or the like; each of R2, R3, and R4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R5 represents a heteroaryl group or the like) or salt thereof.

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1,649-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N643 – PubChem

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Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible and quinolone-resistant gram-positive bacteria, including Streptococcus pneumoniae and MRSA. Analogs 22b, 23c, and 24 demonstrated superior in vitro and in vivo efficacy to ciprofloxacin against these cocci.

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It is an urgent subject to create renewable energy resources such as artificial photosynthetic system and fuel cell free of an environmental pollution, since global warming is closely related to tremendous consumption of fossil fuels to emit carbon dioxide. In this review, we focus on reduction catalyses indispensable for creating new energy systems, especially in the aspects of molecular catalyst. Recent examples of the molecular catalyses for O2, CO2, and H+ reductions are reviewed compared with the characteristics of noble metal catalysts. Molecular aggregates composed of a simple metal complex and a functional polymer can be easily prepared without employing complicated materials such as supra-molecular and hybrid complexes. When using molecular aggregates as a catalyst, the efficient catalysis via an multi-electron transfer reduction by the complex often takes place coupled with the intrinsic characteristics of the polymer employed; moreover, they show unique and active catalysis that cannot be achieved by the corresponding neat complex in a solution or in an electrode-coated state. Typical effects of polymer affecting the efficient molecular catalysis are shown to propose approaches for designing and developing catalysts in molecular level.

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1,37-Naphthyridine – Wikipedia,
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The X-ray crystal structure of N-(7-([2-(dimethylamino)ethyl]amino)-1-methyl-2-oxo-1,2-dihydro-1,6-naphthyridin-3- yl)-3,4,5-trimethoxybenzamide, a potential anticancer agent targeting Hsp90, was established. It crystallizes in the triclinic space group P-1 with cell parameters a = 9.3554(4)A, b = 11.4450(5)A, c = 11.5629(4)A, alpha = 87.140(2), beta = 78.8070(19), gamma = 69.2119(19), V = 1135.21(8)A3 and Z = 2. The crystal structure was refined to final values of R1 = 0.0492 and wR2 = 0.1386. An X-ray crystal structure analysis revealed that each molecule features intermolecular N-H¡¤¡¤¡¤N hydrogen bonds to form dimers.

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Reference of 5423-54-1, 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.5423-54-1, Name is 1,5-Naphthyridin-4-ol, molecular formula is C8H6N2O. In a article£¬once mentioned of 5423-54-1

The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ?2.5 muM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ?400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.

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The FTIR (4000-400cm-1) and the FT-Raman spectra (4000-50cm-1) of 4-Hydroxy-7-methyl-1,8-naphthyridine-3-carboxylic acid are recorded and investigated. The spectra are interpreted using anharmonic frequency computations by VPT2, VSCF and PT2-VSCF methods within DFT/6-311G(d,p) framework. The root mean square (RMS) values indicate that VSCF computed frequencies are in close agreement with the observed frequencies. The combination and overtone bands are also identified in the FTIR spectrum. The intermolecular O-H?O hydrogen bonding interactions are discussed in the dimer structure of the molecule. The magnitudes of the coupling between pair of modes are also computed. The electronic spectra in water and ethanol solvents are analyzed using TD-B3LYP/6-311++G(d,p) level of theory. Molecular electrostatic potential (MEP) and HOMO-LUMO analysis are also performed.

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1,62-Naphthyridine – Wikipedia,
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Reference of 100361-18-0, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 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 Article£¬once mentioned of 100361-18-0

In an attempt to search for clinically useful antitumor agents, we have discovered that a series of 1,7-disubstituted-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids possessed moderate cytotoxic activity. We investigated the structure-activity relationships in this series of compounds by changing N-1 and C-7 positions and the core ring structure itself and evaluated the synthesized compounds against several murine and human tumor cell lines. These modifications led us to the following findings. (1) The 2-thiazolyl group at the N-1 position of the naphthyridine structure is the best substituent for antitumor activity. (2) Regarding core ring structure, the naphthyridine derivative is the most active followed by pyridopyrimidine analogue. (3) At the C-7 position, aminopyrrolidine derivatives are more effective than other amines or thioether derivatives. Finally, the trans-3-amino-4-methoxypyrrolidinyl derivative (43j) and the 3-amino-3-methylpyrrolidinyl derivative (43f) as well as 3-aminopyrrolidinyl derivative (AT-3639, 1) were determined to be effective in in vitro and in vivo antitumor assays, and their activity was comparable to that of etoposide.

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1,742-Naphthyridine – Wikipedia,
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The self-assembly into supramolecular polymers is a process driven by reversible non-covalent interactions between monomers, and gives access to materials applications incorporating mechanical, biological, optical or electronic functionalities. Compared to the achievements in precision polymer synthesis via living and controlled covalent polymerization processes, supramolecular chemists have only just learned how to developed strategies that allow similar control over polymer length, (co)monomer sequence and morphology (random, alternating or blocked ordering). This highlight article discusses the unique opportunities that arise when coassembling multicomponent supramolecular polymers, and focusses on four strategies in order to control the polymer architecture, size, stability and its stimuli-responsive properties: (1) end-capping of supramolecular polymers, (2) biomimetic templated polymerization, (3) controlled selectivity and reactivity in supramolecular copolymerization, and (4) living supramolecular polymerization. In contrast to the traditional focus on equilibrium systems, our emphasis is also on the manipulation of self-assembly kinetics of synthetic supramolecular systems.

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Human telomeric G-quadruplex DNA stabilization has emerged as an exciting novel approach for anticancer drug development. In the present study, we have designed and synthesized three C2-symmetric bisubstituted bisbenzimidazole naphthalenediimide (NDI) ligands, ALI-C3, BBZ-ARO, and BBZ-AROCH2, which stabilize human telomeric G-quadruplex DNA with high affinity. Herein, we have studied the binding affinities and thermodynamic contributions of each of these molecules with G-quadruplex DNA and compared the same to those of the parent NDI analogue, BMSG-SH-3. Results of fluorescence resonance energy transfer and surface plasmon resonance demonstrate that these ligands have a higher affinity for G4-DNA over duplex DNA and induce the formation of a G-quadruplex. The binding equilibrium constants obtained from the microcalorimetry studies of BBZ-ARO, ALI-C3, and BBZ-AROCH2 were 8.47, 6.35, and 3.41 muM, respectively, with h-telo 22-mer quadruplex. These showed 10 and 100 times lower binding affinity with h-telo 12-mer and duplex DNA quadruplexes, respectively. Analysis of the thermodynamic parameters obtained from the microcalorimetry study suggests that interactions were most favorable for BBZ-ARO among all of the synthesized compounds. The DeltaGfree obtained from molecular mechanics Poisson-Boltzmann surface area calculations of molecular dynamics (MD) simulation studies suggest that BBZ-ARO interacted strongly with G4-DNA. MD simulation results showed the highest hydrogen bond occupancy and van der Waals interactions were between the side chains of BBZ-ARO and the DNA grooves. A significant inhibition of telomerase activity (IC50 = 4.56 muM) and induced apoptosis in cancer cell lines by BBZ-ARO suggest that this molecule has the potential to be developed as an anticancer agent.

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1,262-Naphthyridine – Wikipedia,
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Stepwise changes of functional oxo and amino groups in 1,8-naphthyridines to modify the supramolecular architecture have been carried out. The first example of a naphthyridine helix has been found and its structure established by X-ray crystallography. The design is based on hydroxy and amido tautomeric naphthyridines which crystallize in dimers or catemers, one of them attaining helicity. The most stable tautomer present in all the compounds discussed in this paper, as well as the formation of hydrogen-bonded dimers or catemers, was established by X-ray crystallography and rationalized with theoretical calculations.

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1,520-Naphthyridine – Wikipedia,
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