74901-29-4Relevant academic research and scientific papers
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.
Comparing coordination uranyl(vi) complexes with 2-(1: H -imidazo[4,5- b] phenazin-2-yl)phenol and derivatives
Ariyarathna, I. R.,Gorden, A. E. V.,Hardy, E. E.,Hiti, E. A.,Maynard, B. A.,Miliordos, E.,Tutson, C. D.,Wilkinson, G. R.
, p. 11113 - 11122 (2021)
Four derivatives of 2-(1H-imidazo[4,5-b]phenazin-2-yl)phenol have been synthesized and characterized structurally using X-ray crystallography. Coordination complexes with uranyl (UO22+) and copper (Cu2+) were prepared and absorption/emission spectra detailed. We observed increased fluorescence upon uranyl binding, in stark contrast to rapid quenching observed with the addition of copper. These phenomena have been further examined by DFT computational methods.
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.
SMALL MOLECULES TARGETING MUTANT MAMMALIAN PROTEINS
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Paragraph 0649; 0651, (2021/12/03)
Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with a mutation in a protein.
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.
Effects of Substituents on Metastable-State Photoacids: Design, Synthesis, and Evaluation of their Photochemical Properties
Liu, Junning,Tang, Wenqi,Sheng, Lan,Du, Zhen,Zhang, Ting,Su, Xing,Zhang, Sean Xiao-An
supporting information, p. 438 - 445 (2019/01/08)
Recently, metastable-state photoacids have been widely used to control proton transfer in numerous chemical and biological processes as well as applications with visible light. Generally, substituents have a great influence on the photochemical properties of molecules, which will further affect their applications. Yet, the effects of substituents on metastable-state photoacids have not been studied systematically. In this work, 16 metastable-state photoacid derivatives were designed and synthesized on the basis of substituents having a large range of σ–π electron–donor–acceptor capabilities. The effects of substituents on the color display [or maximum absorption band(s)], solubility, pKa values, dark/photoacidity, photosensitivity, and relaxation kinetic(s) were investigated in detail. This study will be helpful for the targeted design and synthesis of promising photoacids and the application of their photocontrolled proton-release processes in functional materials/devices.
Comparative Evaluation of Substituent Effect on the Photochromic Properties of Spiropyrans and Spirooxazines
Balmond, Edward I.,Tautges, Brandon K.,Faulkner, Andrea L.,Or, Victor W.,Hodur, Blanka M.,Shaw, Jared T.,Louie, Angelique Y.
, p. 8744 - 8758 (2016/10/14)
Spiropyrans and spirooxazines represent an important class of photochromic compounds with a wide variety of applications. In order to effectively utilize and design these photoswitches it is desirable to understand how the substituents affect photochromic properties, and how the different structural motifs compare under identical conditions. In this work a small library of photoswitches was synthesized in order to comparatively evaluate the effect of substituent modifications and structure on photochromism. The library was designed to modify positions that were believed to have the greatest effect on C-O bond lability and therefore the photochromic properties. Herein we report a comparative analysis of the UV and visible light responses of 30 spiropyrans, spiroindolinonaphthopyrans, and spirooxazines. The influence of gadolinium(III) binding was also investigated on the library of compounds to determine its effect on photoswitching. Both assays demonstrated different trends in substituent and structural requirements for optimal photochromism.
AMIDINE SUBSTITUTED BETA - LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS
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Paragraph 00235, (2013/08/15)
The present invention relates to novel β-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.
COMPOUNDS AND METHODS
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Page/Page column 110, (2013/03/26)
The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORy.
HETEROCYCLIC COMPOUNDS USEFUL AS ANABOLIC AGENTS FOR LIVESTOCK ANIMALS
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Page/Page column 88, (2008/06/13)
Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.
