79744-64-2Relevant academic research and scientific papers
Determining Essential Requirements for Fluorophore Selection in Various Fluorescence Applications Taking Advantage of Diverse Structure-Fluorescence Information of Chromone Derivatives
Chen, Yikun,Gao, Yongxin,He, Yujun,Zhang, Gang,Wen, Hui,Wang, Yuchen,Wu, Qin-Pei,Cui, Huaqing
, p. 1001 - 1017 (2021/01/09)
Herein, we report our work exploring the essential requirements for fluorophore selection during the development of various fluorescence applications. We assembled a library of chromone-derived fluorophores with diverse structure-fluorescence properties, which allowed us to choose the fluorophore pairs with similar structures but differing fluorescence properties and compared the performance of the selected fluorophore pairs in three types of commonly used fluorescence applications. We found that the selection standard of a suitable fluorophore is variable depending on the application. (1) In fluorescence imaging, fluorophores with strong and constant fluorescence under various conditions, such as a large pH range, are preferred. Notably, (2) in the detection of bioactive species, fluorophores with relatively lower fluorescence quantum yield favor the detection sensitivity. Furthermore, (3) in enzymatic assays employing fluorescence, the key parameter is the binding affinity between the fluorophore and the enzyme.
Synthesis and biological evaluation of novel chromonyl enaminones as α-glucosidase inhibitors
Mendieta-Moctezuma, Aarón,Rugerio-Escalona, Catalina,Villa-Ruano, Nemesio,Gutierrez, Rsuini U.,Jiménez-Montejo, Fabiola E.,Fragoso-Vázquez, M. Jonathan,Correa-Basurto, José,Cruz-López, María C.,Delgado, Francisco,Tamariz, Joaquín
, p. 831 - 848 (2019/04/25)
Series of novel chromonyl enaminones 1a–e and 2a–e and 3-alkylated chromones 3a–e were synthesized and evaluated in vitro as α-glucosidase inhibitors as well as antioxidant and antifungal agents. Antifungal activity was tested on strains of Candida albicans. Compounds 2a and 2d–e showed good inhibition of the α-glucosidase enzyme (IC50 = 5.5, 0.9, and 1.5 mM, respectively), their effect being better than that of 1a–e, 3a–e, and acarbose (the standard, IC50 = 7.73 ± 0.9 mM). The structure–activity relationship suggests that the phenyl group at the C-3 position of the chromone ring system and the 4-chlorophenyl group at the enaminone moiety (derivatives 2) increased the inhibition of α-glucosidase. Compounds 2a–e exhibited a slight antioxidant effect, and compounds 3a–e a moderate antifungal activity against C. albicans (IC50 70.5–83.1 μg/mL). Docking studies revealed that compounds 2 interact with the α-glucosidase residues of the binding pocket. Therefore, these chromone derivatives may be considered as potential α-glucosidase inhibitors, as well as antifungal agents against some Candida strains of yeast.
Compound formed by combining ferulic acid with asarone analogue as well as preparation method and application of compound
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Paragraph 0051; 0052, (2017/04/08)
The invention belongs to the technical field of medicines and discloses a compound formed by combining ferulic acid with an asarone analogue as well as a preparation method and an application of the compound. The structure of the compound is shown in the
