Study On The Synthesis And Bioactivity Of 1, 5-Diaryl-3-pyrazolidinone

Heterocyclic compounds as medicines and pesticides has been developed mostquickly and has become the new trend in the development. In the new developedmedical and pesticidal heterocyclic compounds are the most important domain3-Pyrazolidinones can increase GABA (3,-aminobutyric acid) level in brains ofbeasties, and show anticonvulsant activities of the GABA-T inhibitor.3-Arylpropenates are the one kind of the most important intermediates in thefields of the organic synthesize and which play essential roles in somebiosynthetic and metabolic pathways. In addition, 3-arylpropenates themselveshave attracted increasing interest in connection with their activity as potentinhibitorsof proteolytic enzymes, inhibitors of A4 hydrolase,photopolymerization initiators, and precursors in the asymmetric synthesis of-hydroxy carboxylic acids. In this thesis, the method for preparation of bioactivitycompounds 1,5-diaryl-3- pyrazolidinones has been studied. Their bioactivity hasalso been measured.Perkin reaction is an important traditional 3-arylpropenoic acid synthesismethod. The reaction of benzaldehyde or its analogs and acetic anhydride underthe catalysis of anhydrous potassium carbonate has been studied. 3-arylpropenoicacids {3-(4-fluorophenyl) propenoic acid, 3-(3-benoxyphenyl) propenoic acid }have been synthesized. Their yields are about 50%. And the structures of theseproductions have been confirmed by elemental analyst, IR, 1H-NMR whichshowed that they are 3-arylpropenoic acidsA series of 3-arylpropenates {3-(3,4-dimethoxyphenyl) propenate ,3-(4-fluorophenyl) propenate, 3-(4-chlorophenyl) propenate, 3-(3-benoxyphenyl)propenate et. } have been synthesized by reaction of 3-arylpropenoic acids andabsolute alcohol under the catalysis of p-toluene sulfuric acid. The yield of thisreaction is about 70%. The structures of these productions have been confirmedby elemental analyst, IR, lH-NMR.3-arylpropenates were reacted with hydrazine catalysed by sodiummethylate, which gained 1,5-diaryl-3-pyrazolidinones. Their yields are about50-80%. The structures of these productions have been confirmed by elementalanalyst, IR, 1H-NMR, UV, MS which showed that the structures of thesecompounds are the same as desired.The bioactivitis of 1,5-diaryl-3-pyrazolidinones in this thesis were tested,and it was found that some of them showed good bioactivity...