- Design and Synthesis of Novel c-di-GMP G-Quadruplex Inducers as Bacterial Biofilm Inhibitors
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The formation of biofilms by clinical pathogens typically leads to chronic and recurring antibiotic-resistant infections. High cellular levels of cyclic diguanylate (c-di-GMP), a ubiquitous secondary messenger of bacteria, have been proven to be associate
- Chen, Wei-Min,Lin, Jing,Lin, Qian-Wen,Liu, Jun,Wang, Zi-Qiang,Xuan, Teng-Fei,Yu, Hai-Tao
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p. 11074 - 11089
(2021/08/20)
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- Quinoline aromatic ethylene derivative and applications in preparation of fluorescent dyes and fluorescent probes
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The invention relates to the technical field of nucleic acid detection, particularly to a quinoline aromatic ethylene derivative and applications in preparation of fluorescent dyes and fluorescent probes, wherein the quinoline aromatic ethylene derivative
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Paragraph 0051; 0054; 0055; 0060; 0062; 0065; 0067
(2020/01/12)
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- Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment
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A series of 2-arylethenyl-N-methylquinolinium derivatives were designed and synthesized based on our previous research of 2-arylethenylquinoline analogues as multifunctional agents for the treatment of Alzheimer's disease (AD) (Eur. J. Med. Chem. 2015, 89, 349–361). The results of in vitro biological activity evaluation, including β-amyloid (Aβ) aggregation inhibition, cholinesterase inhibition, and antioxidant activity, showed that introduction of N-methyl in quinoline ring significantly improved the anti-AD potential of compounds. The optimal compound, compound a12, dramatically attenuated the cell death of glutamate-induced HT22 cells by preventing the generation of ROS and increasing the level of GSH. Most importantly, intragastric administration of a12?HAc was well tolerated at doses up to 2000 mg/kg and could traverse blood-brain barrier.
- Xia, Chun-Li,Wang, Ning,Guo, Qian-Liang,Liu, Zhen-Quan,Wu, Jia-Qiang,Huang, Shi-Liang,Ou, Tian-Miao,Tan, Jia-Heng,Wang, Hong-Gen,Li, Ding,Huang, Zhi-Shu
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p. 139 - 153
(2017/03/02)
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- Synthesis, spectroscopy and computational studies of some novel π-conjugated vinyl N-alkylated quinolinium salts and their precursor's
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A series of π-conjugated vinyl N-methylated quinolinium salts (3) and their precursor's N-alkylated quinolinium salts (2) were prepared and characterized by NMR, IR, UV-Vis and MS spectroscopy. It was confirmed that the hydroxyl and amino derivatives of vinyl N-methylated quinolinium salts lead to spiro type compounds (4). The syntheses of N-alkylated quinolinium salts were successful, and even multigram scale was achievable. The structures of 1,2-dimethylquinolinium iodide (2a) and 1-ethyl-2-methylquinolinium iodide (2b) were determined by single crystal X-ray diffraction method. NMR spectra showed readily diagnostic H-1 and C-13 signals from methyl and N-alkyl groups for both 2 and 3. The geometries of the studied compounds were optimized in singlet states using the density functional theory (DFT) method with B3LYP functional. In general, the predicted bond lengths and angles are in a good agreement with the values based on the X-ray crystal structure data.
- Nycz, Jacek E.,Czyz, Karolina,Szala, Marcin,Malecki, Jan G.,Shaw, George,Gilmore, Brendan,Jon, Marek
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p. 416 - 423
(2015/11/27)
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- Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes
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Almond and VolSurf + modelling procedures allowed the structural design of new di- and mono-heteroaryl-ethylenes. The structural modifications suggested by the molecular modelling were verified by the synthesis of the designed molecules and by the evaluation of their in vitro activities against two lung tumour cell lines, A549 and H226. 2-{(E)-2-[5′-(Dibutylamino)-2,2′- bithien-5-yl]vinyl}-1-methylquinolinium iodide exhibited in vitro antiproliferative activity two orders of magnitude higher than that of the most active compound previously synthesized in our laboratory.
- Fortuna, Cosimo G.,Barresi, Vincenza,Bonaccorso, Carmela,Consiglio, Giuseppe,Failla, Salvatore,Trovato-Salinaro, Angela,Musumarra, Giuseppe
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experimental part
p. 221 - 227
(2012/02/15)
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- Solvent-free condensation of methyl pyridinium and quinolinium salts with aldehydes catalyzed by DBU
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Methylpyridinium and methylquinolinium salts were condensed under solvent-free conditions with aromatic aldehydes in the presence of 1,8-diazabicyclo[5.4.]undec-7-ene (DBU) as catalyst, by grinding at room temperature. The products are dyes or useful intermediates. The DBU can be easily recycled and reused. Taylor & Francis Group, LLC.
- Seiad, Linda Loucif,Villemin, Didier,Bar, Nathalie,Hachemi, Messaoud
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experimental part
p. 650 - 657
(2011/12/21)
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- Synthesis, structure and in vitro antibacterial activities of new hybrid disinfectants quaternary ammonium compounds: Pyridinium and quinolinium stilbene benzenesulfonates
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The series of pyridinium (1-10) and quinolinium (11-20) stilbene benzenesulfonates have been synthesized and their structures were investigated by UV-vis, FT-IR and 1H NMR spectroscopy. In addition, compound 5 was also determined by single crystal X-ray diffraction technique. The antibacterial activity of the synthesized compounds against both Gram-positive and Gram-negative bacteria has been determined. The quinolinium derivatives exhibited two very potent characteristic activities, namely, (i) specific activity to Methicillin-Resistant Staphylococcus aureus and (ii) with broad band spectrum activity. Compounds 11, 13 and 14 are the most active showing broad spectrum antibacterial activity against Gram-positive (Methicillin-Resistant S. aureus, S. aureus, Bacillus subtilis, Vancomycin-Resistant Enterococcus faecalis and E. faecalis) and Gram-negative bacterium (Shigella sonnei). The MICs of these compounds were found to be better than that of Benzalkonium chloride (BZK), the commercially used disinfectant. The new pyridinium and quinolinium stilbene benzenesulfonates have been synthesized and characterized. All compounds were evaluated for their antibacterial activity against the tested Gram-positive and Gram-negative bacteria using colorimetric assay.
- Chanawanno, Kullapa,Chantrapromma, Suchada,Anantapong, Theerasak,Kanjana-Opas, Akkharawit,Fun, Hoong-Kun
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experimental part
p. 4199 - 4208
(2010/09/16)
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- Combinatorial approach to organelle-targeted fluorescent library based on the styryl scaffold
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The first fluorescent styryl dye library with a broad color range was synthesized by combinatorial condensation of various aldehydes and methyl pyridinium compounds, and their applications as organelle specific staining probes were demonstrated. Copyright
- Rosania, Gustavo R.,Lee, Jae Wook,Ding, Liang,Yoon, Hai-Shin,Chang, Young-Tae
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p. 1130 - 1131
(2007/10/03)
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