74901-29-4Relevant articles and documents
Selective sensing Ca2+ with a spiropyran-based fluorometric probe
Wang, Li,Yao, Yuanjun,Wang, Jiao,Dong, Chuan,Han, Hui
, p. 707 - 714 (2019)
Spiropyran (SP) and its derivatives operate between their ring opening and closing forms as a versatile molecular platform for the fluorescence detection of cations and anions, using a colour change for signalling. A functionalized SP fluorescence probe, L, was prepared and characterized. Probe L can detect Ca2+ with a fluorescence ‘turn-on’ response in ethanol solution. It selectively binds Ca2+ to form a 1:1 ligand/metal complex, which produced a new emission band centred at 604?nm. The sensing result was clearly observed by the solution colour change from colourless to pink under visible light, and from blue to red under ultraviolet light. The detection limit was calculated to be 4.53?×?10?8?M for Ca2+. The probe provides another possibility that SP-based derivatives could be used for the development and detection of metal ions in environmental and physiological systems.
METHODS OF TREATING CREATINE TRANSPORTER DEFICIENCY
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Paragraph 0510; 0512, (2021/10/02)
Disclosed are methods of treating creatine transporter deficiency, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound that increases transport of a substrate by a mutant or wild-type creatine transporter. Also disclosed are methods of increasing transport of guanidinoacetic acid or a salt thereof across the blood-brain barrier of a mammal, and methods of decreasing accumulation or the concentration of guanidinoacetic acid or a salt thereof in a mammalian cell.
Design, synthesis and biological evaluation of antimicrobial diarylimine and –amine compounds targeting the interaction between the bacterial NusB and NusE proteins
Qiu, Yangyi,Chan, Shu Ting,Lin, Lin,Shek, Tsun Lam,Tsang, Tsz Fung,Barua, Nilakshi,Zhang, Yufeng,Ip, Margaret,Chan, Paul Kay-sheung,Blanchard, Nicolas,Hanquet, Gilles,Zuo, Zhong,Yang, Xiao,Ma, Cong
, p. 214 - 231 (2019/06/14)
Discovery of antimicrobial agents with a novel model of action is in urgent need for the clinical management of multidrug-resistant bacterial infections. Recently, we reported the identification of a first-in-class bacterial ribosomal RNA synthesis inhibitor, which interrupted the interaction between the bacterial transcription factor NusB and NusE. In this study, a series of diaryl derivatives were rationally designed and synthesized based on the previously established pharmacophore model. Inhibitory activity against the NusB-NusE binding, circular dichroism of compound treated NusB, antimicrobial activity, cytotoxicity, hemolytic property and cell permeability using Caco-2 cells were measured. Structure-activity relationship and quantitative structure–activity relationship were also concluded and discussed. Some of the derivatives demonstrated improved antimicrobial activity than the hit compound against a panel of clinically important pathogens, lowering the minimum inhibition concentration to 1–2 μg/mL against Staphylococcus aureus, including clinical strains of methicillin-resistant Staphylococcus aureus at a level comparable to some of the marketed antibiotics. Given the improved antimicrobial activity, specific inhibition of target protein-protein interaction and promising pharmacokinetic properties without significant cytotoxicity, this series of diaryl compounds have high potentials and deserve for further studies towards a new class of antimicrobial agents in the future.
