883-38-5Relevant articles and documents
New hydrazone derivatives of pyrazole-4-carboxaldehydes exhibited anti-inflammatory properties
Chen, Qiuyan,Deng, Xianqing,He, Shihui,Li, Sifan,Liang, Yuqiu,Liu, Bing,Song, Mingxia,Yu, Shengwang
, p. 501 - 510 (2020/04/17)
Background: Several series of hydrazone derivatives of pyrazole-4-carboxaldehydes (4-11) were designed and synthesized to screen their inflammatory activity. Methods: The products were characterized by1H NMR,13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their anti-inflammatory activity. Results and Conclusion: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF-α at the concentration of 10 μg/mL. Compounds 7b and 11c, two of the most potent compounds, exhibited TNF-α inhibitory ability in a dose-dependent manner with IC50 values of 5.56 and 3.69 μM, respectively. In vivo, intraperitoneal administration with 7b and 11c markedly inhibited the ear edema at the doses of 20 and 50 mg/kg. Compound 11c, inhibited edema by 49.59 % at the dose of 20 mg/kg, was comparable to the reference drug dexamethasone at the same dose (with an inhibition of 50.49 %). To understand the binding pattern, molecular docking of representa-tive 7b and 11c was performed, which demonstrated that both compounds have a forceful binding with the TNF-α, and that the phenyl and hydrazide moieties of them play a significant role in binding with the target site.
Synthesis and evaluation of anticonvulsant activities of pyrazol semicarbazones. Part II
Song, Ming-Xia,Wu, Yi,Deng, Xian-Qing
, p. 800 - 808 (2016/09/23)
A series of 2-((5-aryloxy-1-methyl-3-methyl-1H-pyrazol-4-yl)methylene) hydrazinecarboxamides (6a-6l) and 2-((5-aryloxy-1-methyl-3-phenyl-1H-pyrazol-4-yl)methylene) hydrazinecarboxamides (7a-7l) were designed and synthesized. The maximal electroshock shock (MES) and subcutaneous pentylenetetrazole (sc-PTZ) seizure models in mice were used to evaluate the antiepileptic effect of compounds synthesized. Further, the acute neurotoxicity profile was also studied via the rotarod test. The results of sc-PTZ test indicate that a majority of compounds possessed anticonvulsant activity with long duration of protection effects. Among of them, compound 6k was found to be the most promising one, with an ED50 value of 20.4 mg/kg (in sc-PTZ model) and a PI value of 10.8, possessing higher anti-PTZ activity and wider safety margin than valproate and ethosuximide.
Influence of chromophore dipole moments in parameterts of organic light emitting devices based on phenyl and methyl modified pyrazoloquinoline
Gondek,Nizio?,Danel,Szlachcic,Pluciński,Sanetra,Kityk
experimental part, p. 1501 - 1505 (2010/06/20)
Absorption, photo- and electroluminescence spectra of some trityl substituted 1H-pyrazolo[3,4-b]quinolines derivatives (methyl- and phenyl substituted) and fabrication of the single layered organic light emitting diodes are reported. The bulky trityl substituent was introduced to prevent aggregation and crystallization of the dopant in polymer matrix. Role of ground state dipole moments in the observed red Stokes shift, electroluminescent features and photocarrier transport is explored. The maximally achieved brightness about 50 Cd/m2 is observed in the spectral range extending from 443 nm up to 462 nm. The voltage threshold was varied from 7.8 V up to 10 V. The brightness-current dependences show an existence of at least two types of carrier injections.
