Design and Synthesis of GABA Receptor Antagonist Heterocyclic Compounds Belong Pyridones
|School||Wuhan Institute of Technology|
|Keywords||GABA receptors Pyridone Organic Synthesis Pesticides|
In view of the large agricultural country 's basic national conditions , food safety is the most prominent problem , highly toxic pesticides needed alternative varieties In addition, China has joined the WTO , developed with our own intellectual property efficient, safe, economical pesticide varieties is a priority ; due to pest resistance , also in urgent need to develop a novel structure of the pesticides . Based on the above object , the present subject target is a computer-aided drug design designed based on the novel structure of the compound , and by a chemical synthesis method for the synthesis of this series of compounds 1-2 to find the original pesticide lead compounds . within important inhibitory neurotransmitter gamma - aminobutyric acid ( gamma - aminobutyric acid GABA ) as mammalian and insect central nervous system (central nervous system, CNS) , the receptor is an important target is the development of insecticides . Computer the drug aided design ( CADD ) , the difference between the housefly and rat GABA receptor inhibitors pharmacophore model as a design breakthrough point , designed a series of 3 - cyano -1H- pyridone compound . Expect 1-2 insect GABA receptor having selective inhibition of the activity of the lead compound . Successfully synthesized by the three organic synthesis route 14 3 - cyano -1H- pyridine ketones , 13 of which have not been reported , the 14 target compounds were characterized by 1HNMR spectrum , MS and elemental analysis were characterized . The article discusses discussed in part through a set of comparative tests Synthesis Intermediate 3 - phenyl - 4 - N , N - dimethyl -3 - ene-2 ??- one with cyanogen acetamide and N- hydrocarbyl substituted Cyanoacetamide ring Hop mechanism , draw different conclusions of the cyclization direction . The next step will be the target compounds for biological activity test .