- Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
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Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
- Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
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- Sydnones as masked hydrazines for the synthesis of 4-arylazo-1,2-dihydro- pyrazol-3-one derivatives
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A simple and convenient one-pot synthesis of 4-(4-chlorophenylazo)-5- methyl-2-aryl-1,2-dihydro-pyrazol-3-ones (4a-j) has been carried out from 3-arylsydnones (3a-j) by reaction with 2-(4-chlorophenyl)-hydrazono-3-oxo- butyric acid ethyl ester (2b). The 3-arylsydnones are used as masked hydrazines in this reaction. Similarly, the 4-arylazo-2-(7-hydroxy-4-methyl-2-oxo-2H- chromen-8-ylmethyl)-5-methyl-1,2-dihydro-pyrazol-3-ones (7a-j) were synthesized from 3-[(7-acetoxy-4-methyl-8-methylene)coumaryl]sydnone (5). All the newly synthesized compounds exhibited antimicrobial activity greater than the reference drugs used. Copyright Taylor & Francis, Inc.
- Shinge, Prashant S.,Latthe, Prashant R.,Badami, Bharati V.
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p. 2169 - 2176
(2007/10/03)
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- Synthesis, characterization and electrochemical behaviour of some substituted 3-arylazo-8-aldehydo-4-methylcoumarins at dropping mercury and glassy carbon electrodes
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A series of 3-arylazo-8-aldehydo-4-methylcoumarins have been synthesized in excellent yields (80 - 90%) and their structures established on the basis of IR, 1H NMR and elemental analysis. Their purity has been ascertained by chromatographic resolution using acetic acid-toluene (6:4, v/v) as eluent. The electrochemical reduction of 3-arylazo-8-aldehydo-4-methylcoumarins have been studied over a wide pH range at dropping mercury and glassy carbon electrodes. All the compounds found to exhibit well-defined, diffusion-controlled irreversible wave. They give two-electron wave corresponding to the reduction of azo group. On the basis of cyclic voltammetry, coulometry, spectrophotometry, number of protons involved in the rate-determining step, the number of electrons in the reduction and product identification, a plausible reduction mechanism is suggested. Kinetic parameters, i.e. charge-transfer coefficient (αn) and forward rate constant (Kf,h) have also been calculated. The pK values are calculated by polarographic and spectrophotometric method.
- Kumar, Ashok,Sharma, Pratibha,Sharma, Ravi
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p. 363 - 368
(2007/10/03)
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- On the Polarographic Reduction Mechanism of Some Heterocyclic Compounds
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For evaluating the mechanistic steps, position at d.m.e. and assigning inner or outer sphere path of electrode processes of a number of pyrazole derivatives, thiazoles and their precursors experiments were carried out in the absence and presence of surfactants.All the compounds gave diffusion-controlled, irreversible waves over the entire pH range (2.0-11.0) studied.In presence of surfactants also, diffusion-controlled but more irreversible waves were obtained.In absence and presence of surfactant (CTAB) values of Kapp and αapp for all these compounds were calculated and have been taken as a proof of inner sphere or outer sphere path of the electrode reaction.Results have been explained on the basis of formation of phenylazo-functionalised surfactant as an intermediate species.
- Malik, Wahid U.,Jain, Rajeev
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p. 191 - 194
(2007/10/02)
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