474938-30-2Relevant academic research and scientific papers
Novel heterocycles containing the pyrazole unit
Svetlik, Jan,Liptaj, Tibor
, p. 1260 - 1265 (2002)
New condensed pyrazolo[1,5-e][1,3,5]benzoxadiazocine and bridged 5,11-methano-[1,2,4]triazolo[1,2-c]-[1,3,4]benzoxadiazepine heterocyclic ring systems were prepared by cyclizations of 4,5-dihydro-3-methyl-5-(2-hydroxyphenyl)-1H-pyrazole-1-carboximidamide
Novel 2-(benzo[d]thiazol-2-yl)-1-(3-methyl-5-substituted-phenyl-4,5- dihydropyrazol-1-yl)ethanone Derivatives: Synthesis and antibacterial activity
Pan, Chun-Xiu,Lia, Jun,Liu, Xin-Hua
experimental part, p. 459 - 463 (2012/06/15)
A series of novel 2-(benzo[d]thiazol-2-yl)-1-(3-methyl-5-substituted- phenyl-4,5-dihydropyrazol-1-yl)ethanone derivatives were synthesized and characterized by NMR, ESI-MS. Biological activity tests results show that compounds 4a, 4b, 4d and 4g displayed activity with MIC of 1.562 ?g/mL against B. subtilis ATCC 6633, compound 4d displayed significant activity with MIC of 1.562 μg/mL against S. aureus ATCC 6538. Compound 4a with potent antibacterial activities strongly inhibited S. aureus DNA gyrase and B. subtilis DNA gyrase with IC50s of 0.5 μg/ml against S. aureus DNA gyrase and B. subtilis DNA gyrase.
Synthesis and molecular docking studies of novel 2-chloro-pyridine derivatives containing flavone moieties as potential antitumor agents
Liu, Xin-Hua,Liu, Hui-Feng,Shen, Xu,Song, Bao-An,Bhadury, Pinaki S.,Zhu, Hai-Liang,Liu, Jin-Xing,Qi, Xing-Bao
scheme or table, p. 4163 - 4167 (2010/08/20)
A series of novel 2-chloro-pyridine derivatives containing flavone, chrome or dihydropyrazole moieties as potential telomerase inhibitors were synthesized. The bioassay tests showed that compounds 6e and 6f exhibited some effect against gastric cancer cell SGC-7901 with IC50 values of 22.28 ± 6.26 and 18.45 ± 2.79 μg/mL, respectively. All title compounds were assayed for telomerase inhibition by a modified TRAP assay, the results showed that compound 6e can strongly inhibit telomerase with IC50 value of 0.8 ± 0.07 μM. Docking simulation was performed to position compound 6e into the active site of telomerase (3DU6) to determine the probable binding model.
Synthesis, structure, and antibacterial activity of novel 5-arylpyrazole derivatives
Liu, Xin-Hua,Lv, Peng-Cheng,Li, Bo,Zhu, Hai-Liang,Song, Bao-An
, p. 223 - 230 (2008/09/18)
A series of novel 1-(acetyl,carboxamide,carbothioamide)substituted-5- (substituted-phenyl)-3-methy-4,5-dihydropyrazole derivatives have been synthesized and characterized by 1H NMR, IR, ESI-MS, and elemental analysis. Compounds 6h and 6q were further characterized by single crystal X-ray structural analysis. All of the compounds have been screened for their antibacterial potential in vitro against Bacillus subtilis ATCC 6633, Escherichia coli ATCC 35218, Pseudomonas fluorescens ATCC 13525, and Staphylococcus aureus ATCC 6538. Among the tested compounds, some of them display significant activity against the tested strains, and compounds 5ac and 6h show potent activity with a minimum inhibitory concentration value of 1.562 ?g mL?1 against B. subtilis ATCC 6633, which is comparable to the positive control penicillin. Structure?effect relationships are also discussed based on the experimental data. CSIRO 2008.
