Dissertation > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry

Design and Synthesis of GABA Receptor Antagonist Heterocyclic Compounds Belong Pyridones

Author HuangLong
Tutor JuXiuLian
School Wuhan Institute of Technology
Course Biochemical Engineering
Keywords GABA receptors Pyridone Organic Synthesis Pesticides
CLC R914
Type Master's thesis
Year 2010
Downloads 58
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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 .

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