Egypt
Research Article
Design, Synthesis, In Vivo Anti-inflammatory, Analgesic Activities and Molecular Docking of Some Novel Pyrazolone Derivatives
Author(s): Ahmad Farouk Eweas, Ahmed OH El-Nezhawy, Rehab Fawzy Abdel-Rahman and Ayman R BaiuomyAhmad Farouk Eweas, Ahmed OH El-Nezhawy, Rehab Fawzy Abdel-Rahman and Ayman R Baiuomy
A novel series of 1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one derivatives were synthesized. The synthesis started with the important building block 3, which was prepared via coupling of from 2-(bi's (methylthio) methylene) malononitrile 1 with 4-amino-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one 2. The 5-aminopyrazole derivatives 4-8 were prepared from the cyclocondensationof 3 with the appropriate sulfonohydrazides and pyridine- 4-carbohydrazide respectively. Cyclocondensation of 1 or 9 with pyridine-4-carbohydrazide and 4-methylbenzene sulfonohydrazide corresponding pyrazole derivatives 10, 11, 12 and 13. Condensation 2 and 1-isothiocyanato-4- methylbenzene 14 yielded 15 which was refluxed with malonic acid to yielded1-(1,5-dimethyl-3-oxo-2-phenyl-2,3- dihydro-1H-pyrazol-4-yl)-2-thioxo-3-(2methylphenyl) dihydropyrimidine-4,6(1H,5H)-dione (16). All t.. Read More»
DOI:
10.4172/2161-0444.1000301
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