1051373-06-8Relevant articles and documents
Azetidine-Containing Heterospirocycles Enhance the Performance of Fluorophores
Zhou, Junliang,Lin, Xianfeng,Ji, Xin,Xu, Shuang,Liu, Chang,Dong, Xiaochun,Zhao, Weili,Zhao, Weili
, p. 4413 - 4417 (2020)
Fluorescent dyes are extensively utilized in various fluorescence imaging techniques. However, many existing modification strategies could not balance the performance (such as brightness, photostability, water solubility, and permeability) of fluorophores. Herein we report a general strategy to enhance the performance of donor-acceptor-type fluorophores by introducing azetidine-containing heterospirocycles to the commonly used fluorophore scaffolds. Such a strategy turned out to be a general way to develop high-quality fluorophores.
Modification of the Thioglycosyl-Naphthalimides as Potent and Selective Human O-GlcNAcase Inhibitors
Shen, Shengqiang,Dong, Lili,Chen, Wei,Zeng, Xiangdi,Lu, Huizhe,Yang, Qing,Zhang, Jianjun
, p. 1241 - 1246 (2018)
β-N-Acetylhexosaminidases are widely distributed exoglycosidases and have attracted significant attention due to their important roles in the field of pesticide and drug discovery. Remarkably, human O-GlcNAcase (hOGA) and human β-N-acetylhexosaminidase (HsHex) possess the same catalytic mechanism but play different physiological actions in vivo. In this Letter, we aim to improve the inhibitory potency and selectivity of previously reported thioglycosyl-naphthalimides against hOGA. The rational compound design led to the synthesis of 13r bearing a 4-piperidylnaphthalimide moiety as a highly potent hOGA inhibitor (Ki = 0.6 μM against hOGA) with good selectivity (Ki > 100 μM against HsHexB). Furthermore, to investigate the basis for the potency and selectivity of 13r against hOGA, the possible inhibitory mechanisms of selected inhibitors (15b, 13b, and 13r) against hOGA and HsHexB were studied using molecular docking and MD simulations. These 4-substituted naphthalimide thioglycosides may potentially serve as useful tools for the further study of the function of hOGA.
Novel side-chain alternative copolymer combined FRET and DRET with large pseudo-Stokes shift and polarity-sensitive fluorescence behavior
Yu, Yan,Yang, Bohao,Yuan, Yongjie,Zhang, Hailiang
, p. 11285 - 11292 (2019)
A novel alternative copolymer incorporating tetraphenylethene (TPE) and naphthalimide (NI) into styrene and maleic anhydride as side chains was designed and synthesized. Attributed to the TPE units acting both as emissive donor in the aggregation state an
NAPHTHALENE MONOIMIDE COMPOUNDS AND METHODS THEREOF
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Paragraph 0140; 0150, (2022/02/05)
The present disclosure discloses a compound of Formula (I) and its polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof and a process of preparation of compounds of Formula (
Naphthalimide and quinoline derivatives as inhibitors for insect N-acetyl-β-D-hexosaminidase
Yang, Huibin,Qi, Huitang,Liu, Tian,Shao, Xusheng,Yang, Qing,Qian, Xuhong
, p. 977 - 980 (2019/02/13)
Insect chitinolytic β-N-acetyl-D-hexosaminidase, such as OfHex1 from Ostrinia furnacalis, is a potential target for insecticide design. Among the known OfHex1 inhibitors, Q2 is of great interest because it is the first non-carbohydrate inhibitor. In this study, we designed and synthesized a series of Q2 derivatives by replacing the thiadiazole and naphthalimide groups and changing the linker length. Compound 3m showed the best inhibitory activity with a Ki value of 0.34 μmol/L against OfHex1, which is about one-quarter that of Q2 (Ki = 1.4 μmol/L). Compound 6a showed the best inhibitory activity among the quinoline-containing derivatives (Ki = 2.3 μmol/L). Molecular docking indicated that although 3m, 6a, and Q2 binding the active pocket of OfHex1 in similar mode, compound 3m engaged better than the other compounds in intermolecular interaction with OfHex1.
METHODS FOR OBTAINING COLORED OR CHROMIC SUBSTRATES
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Page/Page column 7; 22, (2018/01/17)
The present invention provides a post-fabrication modification approach for the fabrication of colored and chromic materials and sensors using plasma surface modification to covalently bind the coloring agent to the substrate, thus avoiding leaching of th
Water soluble mitochondrial targeting imaging probe and preparation method thereof
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Paragraph 0117; 0118, (2016/10/10)
The invention discloses a water soluble mitochondrial targeting imaging probe and a preparation method thereof. The structural formula of compounds that form the water soluble mitochondrial targeting imaging probe can be formula (I), (II), (III), (IV), (V
Development of unsymmetrical dyads as potent noncarbohydrate-based inhibitors against human β-N-acetyl-D-hexosaminidase
Guo, Peng,Chen, Qi,Liu, Tian,Xu, Lin,Yang, Qing,Qian, Xuhong
supporting information, p. 527 - 531 (2013/07/26)
Human β-N-acetyl-D-hexosaminidase has gained much attention due to its roles in several pathological processes and been considered as potential targets for disease therapy. A novel and efficient skeleton, which was an unsymmetrical dyad containing naphthalimide and methoxyphenyl moieties with an alkylamine spacer linkage as a noncarbohydrate-based inhibitor, was synthesized, and the activities were valuated against human β-N-acetyl-D- hexosaminidase. The most potent inhibitor exhibits high inhibitory activity with Ki values of 0.63 μM. The straightforward synthetic manners of these unsymmetrical dyads and understanding of the binding model could be advantageous for further structure optimization and development of new therapeutic agents for Hex-related diseases.
Novel naphthalimide-indomethacin hybrids as potential antitumor agents: Effects of linkers on hypoxic/oxic cytotoxicity and apoptosis-inducing activity
Wu, Aibin,Xu, Yufang,Qian, Xuhong
experimental part, p. 893 - 899 (2011/07/08)
A series of novel naphthalimide-indomethacin hybrids with different linkers were designed and synthesized. Their antitumor activity was evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8, and A375 cancer cell lines in vitro. Preliminary results showe
Synthesis of novel multi-chromophoric soluble perylene derivatives and their photosensitizing properties with wide spectral response for SnO2 nanoporous electrode
Tian,Liu,Zhu,Gao,Wu,Cai
, p. 2708 - 2715 (2007/10/03)
Two series of new multi-chromophoric perylene-3,4:9,10-tetracarboxylic dianhydride dyes for solar cell sensitizers have been synthesized. One series consists of oxadiazole or naphthaldicarboximide that are linked with perylene units as N,N'-substituted chromophores. The other series has four substituents in the bay-region of the perylene core in addition to N,N'-substituents. These novel routes to highly efficient sensitizers for Gratzel-type solar cells avoid the complication of doping. A wide spectral photoresponse (from 310 to 700 nm) was observed with maximum IPCE (incident photon-to-current efficiency) of 24%. In addition, the sensitization is dependent on the energy match of the energy bands of the semiconductor and the redox potential of the segments in such assembled dyes.
