580-16-5Relevant articles and documents
Design, synthesis and biological evaluation of novel quinoline-based carboxylic hydrazides as anti-tubercular agents
Chander, Subhash,Ashok, Penta,Cappoen, Davie,Cos, Paul,Murugesan, Sankaranarayanan
, p. 585 - 591 (2016)
In this study, seventeen novel quinoline-based carboxylic hydrazides were designed as potential anti-tubercular agents using molecular hybridization approach and evaluated in-silico for drug-likeness behavior. The compounds were synthesized, purified, and characterized using spectral techniques (like FTIR, 1H NMR, and Mass). The in-vitro anti-tubercular activity (against Mycobacterium tuberculosisH37Ra) and cytotoxicity against human lung fibroblast cells were studied. Among the tested hydrazides, four compounds (6h, 6j, 6l, and 6m) exhibited significant anti-tubercular activity with MIC values below 20?μg/mL. The two most potent compounds of the series, 6j and 6m exhibited MIC values 7.70 and 7.13?μg/mL, respectively, against M.?tuberculosis with selectivity index >26. Structure–activity relationship studies were performed for the tested compounds in order to explore the effect of substitution pattern on the anti-tubercular activity of the synthesized compounds.
Biocatalytic Cross-Coupling of Aryl Halides with a Genetically Engineered Photosensitizer Artificial Dehalogenase
Fu, Yu,Huang, Jian,Wu, Yuzhou,Liu, Xiaohong,Zhong, Fangrui,Wang, Jiangyun
supporting information, p. 617 - 622 (2021/02/03)
Devising artificial photoenzymes for abiological bond-forming reactions is of high synthetic value but also a tremendous challenge. Disclosed herein is the first photobiocatalytic cross-coupling of aryl halides enabled by a designer artificial dehalogenase, which features a genetically encoded benzophenone chromophore and site-specifically modified synthetic NiII(bpy) cofactor with tunable proximity to streamline the dual catalysis. Transient absorption studies suggest the likelihood of energy transfer activation in the elementary organometallic event. This design strategy is viable to significantly expand the catalytic repertoire of artificial photoenzymes for useful organic transformations.
Application of Electron-Rich Covalent Organic Frameworks COF-JLU25 for Photocatalytic Aerobic Oxidative Hydroxylation of Arylboronic Acids to Phenols
Xiao, Guangjun,Li, Wenqian,Chen, Tao,Hu, Wei-Bo,Yang, Hui,Liu, Yahu A.,Wen, Ke
supporting information, p. 3986 - 3991 (2021/03/29)
Visible-light-driven organic reactions are environmentally friendly green chemical transformations among which photosynthetic oxidative hydroxylation of arylboronic acids to phenols has attracted increasing research interest during the very recent years. Given the efficiency and reusability of heterogeneous catalysts, COF-JLU25, an electron-rich COF-based photocatalyst constructed by integrating electron-donating blocks 1,3,6,8-tetrakis(4-aminophenyl)pyrene (PyTA) and 4-[4-(4-formylmethyl)-2,5-dimethoxyphenyl] benzaldehyde (TpDA), was selected as a photocatalyst for the oxidative hydroxylation of arylboronic acids. In our studies, COF-JLU25 demonstrated excellent photocatalytic activity with high efficiency, robust reusability, and low catalyst loading, showcasing an application potential of previously underexplored COF-based photocatalyst composed solely of electron-rich units.
Cu(I)/sucrose-catalyzed hydroxylation of arenes in water: The dual role of sucrose
Murata, Shigeo,Takagi, Mio,Takita, Ryo,Watanabe, Ayako,Watanabe, Kohei
supporting information, p. 7827 - 7831 (2020/11/02)
A protocol for the hydroxylation of aryl halides catalyzed by copper(I) and sucrose in neat water has been developed. The dual role of sucrose, the reaction pathway, and the high selectivity for hydroxylation were investigated using a combination of experimental and theoretical techniques. This journal is