76008-04-3Relevant academic research and scientific papers
A real-time fluorescent sensor specific to Mg2+: Crystallographic evidence, DFT calculation and its use for quantitative determination of magnesium in drinking water
Men, Guangwen,Chen, Chunrong,Zhang, Shitong,Liang, Chunshuang,Wang, Ying,Deng, Mengyu,Shang, Hongxing,Yang, Bing,Jiang, Shimei
, p. 2755 - 2762 (2015)
An off-the-shelf fluorescence turn-on Mg2+ chemosensor 3,5-dichlorosalicylaldehyde (BCSA) was rationally designed and developed. This proposed sensor works based on Mg2+-induced formation of the 2:1 BCSA-Mg2+ complex. The coordination of BCSA to Mg2+ increases its structural rigidity generating a chelation-enhanced fluorescence (CHEF) effect which was confirmed by single crystal XRD studies of the BCSA-Mg2+ complex and TD/DFT calculations. This sensor exhibits high sensitivity and selectivity for the quantitative monitoring of Mg2+ with a wide detection range (0-40 μM), a low detection limit (2.89 × 10-7 mol L-1) and a short response time (2+. Consequently, this fluorescent sensor can be utilized to monitor Mg2+ in real time within actual samples from drinking water. This journal is
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0136; 0137; 0138; 0139; 0778; 0779; 0780; 0781, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
Optimization of a binding fragment targeting the “enlarged methionine pocket” leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors
Huang, Wenlin,Zhang, Zhongsheng,Ranade, Ranae M.,Gillespie, J. Robert,Barros-álvarez, Ximena,Creason, Sharon A.,Shibata, Sayaka,Verlinde, Christophe L.M.J.,Hol, Wim G.J.,Buckner, Frederick S.,Fan, Erkang
supporting information, p. 2702 - 2707 (2017/05/29)
Potent inhibitors of Trypanosoma brucei methionyl-tRNA synthetase were previously designed using a structure-guided approach. Compounds 1 and 2 were the most active compounds in the cyclic and linear linker series, respectively. To further improve cellular potency, SAR investigation of a binding fragment targeting the “enlarged methionine pocket” (EMP) was performed. The optimization led to the identification of a 6,8-dichloro-tetrahydroquinoline ring as a favorable fragment to bind the EMP. Replacement of 3,5-dichloro-benzyl group (the EMP binding fragment) of inhibitor 2 using this tetrahydroquinoline fragment resulted in compound 13, that exhibited an EC50 of 4?nM.
Metabolic investigation on ZL006 for the discovery of a potent prodrug for the treatment of cerebral ischemia
Chen, Dongyin,Zhao, Ting,Ni, Kaidong,Dai, Peng,Yang, Lei,Xu, Yi,Li, Fei
supporting information, p. 2152 - 2155 (2016/04/20)
4-((3,5-Dichloro-2-hydroxybenzyl)amino)-2-hydroxybenzoic acid (ZL006, 1) is a small-molecular inhibitor of the nNOS/PSD-95 interaction, that is under preclinical evaluation stage for cerebral ischemia. However, the fast metabolism and low permeability acr
Silver(I)-catalyzed route to pyrroles: Synthesis of halogenated pseudilins as allosteric inhibitors for myosin atpase and x-ray crystal structures of the protein-inhibitor complexes
Martin, Rene,Risacher, Celia,Barthel, Andre,Jaeger, Anne,Schmidt, Arndt W.,Richter, Sabine,Boehl, Markus,Preller, Matthias,Chinthalapudi, Krishna,Manstein, Dietmar J.,Gutzeit, Herwig O.,Knoelker, Hans-Joachim
, p. 4487 - 4505 (2014/08/05)
The pentahalogenated 2-arylpyrrole-type alkaloids pentabromopseudilin and pentachloropseudilin represent a new class of isoform-specific allosteric inhibitors of myosin ATPase. Herein, we describe an application of the silver(I)-catalyzed cycloisomerizati
NITROGENOUS CYCLIC KETONE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page 72-73, (2010/02/08)
A novel compound represented by the formula (I): wherein rings A and B each represents an optionally substituted aromatic ring, or rings A and B may be bonded to each other through linking between bonds or substituents thereof to form a ring; ring C represents a nitrogenous saturated heterocycle optionally having one or more substituents besides the oxo (provided that 2,3-dioxopyrrolidine ring is excluded); R1 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and-------- indicates a single bond or a double bond. It has high antagonistic activity against a tachykinin receptor, especially an SP receptor.
