1237-49-6Relevant academic research and scientific papers
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents
Zhang, Tian-Yi,Zheng, Chang-Ji,Wu, Jie,Sun, Liang-Peng,Piao, Hu-Ri
supporting information, p. 1079 - 1084 (2019/03/06)
Three novel series of dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1–64 μg/mL. Compounds 4b and 4c presented the most potent inhibitory activity against Gram-positive bacteria (S. aureus 4220, MRSA 3167, QRSA 3519) and Gram-negative bacteria (E. coli 1924), with minimum inhibitory concentration values of 1 or 2 μg/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. The cytotoxic activity of the compounds 4a, 4b, 4c and 11n were assessed in L02 cells. In vitro enzyme study implied that compound 4c exerted its antibacterial activity through DHFR inhibition.
Synthesis and the interaction of 2-(1H-pyrazol-4-yl)-1H-imidazo[4,5-f][1,10]phenanthrolines with telomeric DNA as lung cancer inhibitors
Liu, Jiachun,Chen, Mei,Wang, Yanli,Zhao, Xiaoyin,Wang, Sijia,Wu, Yanling,Zhang, Wen
, p. 36 - 49 (2017/04/06)
A novel series of 2-(1H-pyrazol-4-yl)-1H-imidazo[4,5-f][1,10]phenanthrolines were designed, synthesized and evaluated for their antitumor activity against lung adenocarcinoma by CCK-8 assay, electrophoretic mobility shift assay (EMSA), UV-melting study, wound healing assay and docking study. These compounds showed good inhibitory activities against lung adenocarcinoma. Especially compound 12c exhibited potential antiproliferative activity against A549?cell line with the half maximal inhibitory concentration (IC50) value of 1.48?μM, which was a more potent inhibitor than cisplatin (IC50?=?12.08?μM) and leading compound 2 (IC50?=?1.69?μM), and the maximum cell inhibitory rate being up to 98.40%. Moreover, further experiments demonstrated that compounds 12a–d can strongly interact with telomeric DNA to stabilize G-quadruplex DNA with increased ΔTm values from 12.44 to 20.54?°C at a ratio of DNA to compound 1:10. These results implied that growth inhibition of A549?cells mediated by these phenanthroline derivatives is possibly positively correlated to the fact their interaction with telomeric G-quadruplexs.
Synthesis and antimicrobial evaluation of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives
Wei, Zhi-Yu,Liu, Jia-Chun,Zhang, Wen,Li, Ya-Ru,Li, Chao,Zheng, Chang-Ji,Piao, Hu-Ri
, p. 751 - 759 (2016/11/29)
Background: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel ant
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents
Li, Ya-Ru,Li, Chao,Liu, Jia-Chun,Guo, Meng,Zhang, Tian-Yi,Sun, Liang-Peng,Zheng, Chang-Ji,Piao, Hu-Ri
, p. 5052 - 5057 (2015/11/09)
Three series of 1,3-diaryl pyrazole derivatives bearing aminoguanidine or furan-2-carbohydrazide moieties have been synthesized, characterized and evaluated for antibacterial and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1-64 μg/mL. Compounds 6g, 6l and 7l presented the most potent inhibitory activity against Gram-positive bacteria (e.g. Staphylococcus aureus 4220), Gram-negative bacteria (e.g. Escherichia coli 1924) and the fungus, Candida albicans 7535, with minimum inhibitory concentration values of 1 or 2 μg/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. Furthermore, compound 7l showed the greatest anti-inflammatory activity (93.59% inhibition, 30 min after intraperitoneal administration), which was more potent than the reference drugs ibuprofen and indomethacin.
Efficient and highly aldehyde selective wacker oxidation
Teo, Peili,Wickens, Zachary K.,Dong, Guangbin,Grubbs, Robert H.
supporting information; experimental part, p. 3237 - 3239 (2012/08/27)
A method for efficient and aldehyde-selective Wacker oxidation of aryl-substituted olefins using PdCl2(MeCN)2, 1,4-benzoquinone, and t-BuOH in air is described. Up to a 96% yield of aldehyde can be obtained, and up to 99% selectivity can be achieved with styrene-related substrates.
