39175-64-9Relevant academic research and scientific papers
Synthesis and anti-influenza activities of novel baicalein analogs
Chung, Shu-Ting,Chien, Pei-Yu,Huang, Wen-Hsin,Yao, Chen-Wen,Lee, An-Rong
, p. 415 - 421 (2014/05/20)
A series of novel flavones derivatives were synthesized based on modification of the active ingredients of a traditional Chinese medicine Scutellaria baicalensis GEORGI and screened for anti-influenza activity. The synthetic baicalein (flavone) analogs, especially with the B-rings substituted with bromine atoms, were much more potent than oseltamivir or ribavirin against H1N1 Tamiflu-resistant (H1N1 TR) virus and usually with more favorable selectivity. The most promising were 5b, 5c, 6b and 6c, all displaying an 50% effective concentration (EC50) at around 4.0-4.5 μM, and a selective index (SI=50% cytotoxic concentration (CC50)/EC 50)>70. For seasonal H3N2-infected influenza virus, both 5a and 5b with SI >17.3 indicated superior to ribavirin. The flavonoids having both not-naturally-occurring bromo-substituted B-rings and appropriate hydroxyls positioning on the A-rings might be critical in determining the activity and selectivity against H1N1-Tamiflu-resistant infected influenza viruses.
Synthesis and anti-angiogenetic activity evaluation of N-(3-aryl acryloyl)aminosaccharide derivatives
Liu, Kun,Yao, Shuowei,Lou, Yinghan,Xu, Yungen
, p. 83 - 92 (2013/10/21)
In order to find novel potent inhibitors for signal pathways of FGF/FGFR, nineteen N-(3-aryl acryloyl)aminosaccharide derivatives were designed and synthesized based on the binding sites of FGF and oligosaccharides of heparin. Their structures were confirmed by IR, 1H NMR, 13C NMR, MS and elemental analysis. The nineteen target compounds were evaluated for biological activity against HUVEC cell. In vitro assays showed that compound 10s (IC50 = 5.3 μM) exhibited comparable inhibitory effects on endothelial cell growth with topotecan (IC50 = 2.7 μM). Compound 10s (10 μg/egg) also showed obvious anti-angiogenetic activity in the in vivo chicken chorio allantoic membrane (CAM) assay, and the potency was similar to topotecan (10 μg/egg).
Design, synthesis and in vitro antibacterial/antifungal evaluation of novel 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid derivatives
Yu, Zhiyi,Shi, Guanying,Sun, Qiu,Jin, Hong,Teng, Yun,Tao, Ke,Zhou, Guoping,Liu, Wei,Wen, Fang,Hou, Taiping
experimental part, p. 4726 - 4733 (2010/01/06)
A series of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid (norfloxacin) derivatives were prepared according to the principle of combinating bioactive substructures and tested for their activities against five plant pathogenic bacteria and three fungi in vitro. The preliminary bioassays indicated that almost all synthesized target compounds retained the antibacterial activities of norfloxacin and had some antifungal activities as carboxylic acid amide compounds. The activities of compounds 1 and 22 against Xanthomonas oryzae were better than norfloxacin and all tested compounds had better antibacterial activities as compared to the agricultural streptomycin sulfate (a commercial bactericide) against X. oryzae, Xanthomonas axonopodis and Erwinia aroideae. Additionally, compounds 2 and 20 displayed good antifungal activities against Rhizoctonia solani and their inhibition of growth reached 83% and 94% respectively at the concentration of 200 mg/L.
Synthesis of quaternary salts of ammonia from cinnamic acids and their plant growth retardant activity
Sharma,Kaur, Sukhvir
, p. 612 - 614 (2008/12/20)
A series of N,N-dimethyl-N-benzyl ammonium chloride cinnamides (1a-e) were prepared from the reaction between cinnamyl chlorides (4a-e) and N,N-dimethylphenylmethanamines (6a-e). These salts were tested for their biological activity on germination, seedling growth and adventitious root formation on hypocotyl cuttings of Vigina radiata (SML-668) and were found to be markedly inhibit germination and seedling growth of mungbean seeds under laboratory conditions.
Synthesis of N-[4-(propyl)cyclohexyl]-amides with anti-inflammatory and analgesic activities
Pau, Amedeo,Boatto, Gianpiero,Asproni, Battistina,Palomba, Michele,Auzzas, Luciana,Cerri, Riccardo,Palagiano, Francesco,Filippelli, Walter,Falcone, Giuseppe,Motola, Giulia
, p. 439 - 447 (2007/10/03)
Seventeen (un)substituted N-[4-(propyl)cyclohexyl]-amides (6a-h, 7a-h and 8) were synthesized and tested as anti-inflammatory and analgesic agents. The substituents on the aromatic ring were chosen in order to study the influence of electron-withdrawing or electron-donating residues, that change the electronic density on the aromatic moiety. The pharmacological results allow drawing some preliminary considerations on structure-activity relationships. (C) 2000 Elsevier Science S.A.
