Design And Synthesis Of GABA Receptor Antagonist Heterocyclic Compounds Belong Pyridones

According to the basic condition of our country, food safety is the most outstanding problem in china. High toxic pesticides need to change, for another reason, since our Country has entered WTO, developing high efficiency, safety and economy pesticides with own intellectual property rights has become one of the most urgent affairs of our country; Because of the resistance to drugs of pests, new structure pesticides are also been needed. From the foregoing reason, the target of this taskproblem is to synthetize series of new compounds on the basis of Computer-aided drug design in the hope of finding 1-2 original pesticide leading compounds.γ-Aminobutyric Acid receptor is one of the most important targets of pesticides, which has been discovered in the middle of 1980s. For the example of pesticide plants avermectin, antibiotics avermectin and fipronil which are all act on GABA receptor. GABA receptor's inhibitors insecticides with a huge development potential.For screening efficiency, safety and specificity of new pesticide pyridine ketone heterocyclic compounds, based on the computer-aided drug design we simulated some compounds with potential GABA receptors bioactivity, those compounds were synthesized through three routes to get fourteen 3-cyano-1H-pyridone compounds, all of the fourteen compounds have been characterized by EI-MS, 1H NMR spectra and elemental analysis.The mechanisms of cyclization have been discussed in the discussion section due to a pair of contrastive experiments. Biological activity assay of the target compounds which have been synthesized is the following task.