Dissertation > Excellent graduate degree dissertation topics show

Studies on Biological Activities Molecule with Piperidine Ring

Author: ZhangJianGe
Tutor: WenRen
School: Fudan University
Course: Medicinal Chemistry
Keywords: piperidine nipecotic acid 1-benzylidene-1,2,3,4-tetra-hydroisoquinoline alkaloids GAT-1 anti-epileptics Wittig reaction asymmetric hydrogenation
CLC: R914
Type: PhD thesis
Year: 2005
Downloads: 367
Quote: 1
Read: Download Dissertation

Abstract


No matter natural or synthetic piperidine derivatives exhibit an extensive range of biological activities such as anti-tumor, anti-inflammatory, anxiolytics, anti-epileptics. Piperidine is a normal constituent in mammalian brain, affects synaptic mechanism in the CNS. Nipecotic acid display in vitro as inhibitors of [3H]-GABA transporters. GABA transporters are important therapeutical targets in epilepsy and potentially other neurological diseases related to the GABA system. The selective inhibitors of GABA transporters can enhance GABA concentration of synapse so as to be a major enhancement of GABA ergic neurotransmission function. It is hopeful to develop relevant treatment medicine of disease relative to GABA ergic neurotransmission such as anti-epileptics, anti-convulsion, and analgesics.It was found that the piperidine derivatives possessed potent inhibitory activity of GAT-1 but seldom found the publications in China. In order to further study on the selective inhibitors of GABA transports, GAT-1 was regarded as biological targets in our research. Tiagabine and NNC-711 were selected to be lead compounds so as to design and synthesize a series of synthetic piperidine derivatives and study their biological activities. On the other hand, a series of organic sulfur compounds were designed and synthesized by sulfur atom in the chain instead of a methylene group of Tiagabine, and sulfur ether compounds further oxidized. The inhibited activities of GABA transporters of these new organic sulfur compounds were tested in vitro. Reticuline is a natured isoquinoline alkaloid with many important biological activities, especially biological activity in CNS. Reticuline can be regarded as a lead compound to design and synthesize a series of natural piperidine derivatives. The [3H]-GABA uptake inhibition bioassays of all synthetic compounds were done in Institute of Shanghai Institutes of Cell biology & Biochemistry.During our studies, 166 compounds, including 53 target compounds, were synthesized. Among the 166 compounds, 112 are new compounds.

Related Dissertations

  1. Homoisoflavonoids from Ophiopogon Japonicus and Alkaloids from Elaeocarpus Sphaericus,R284.1
  2. Dark purple Fritillaria medicinal active ingredient extraction technology and the chemical composition of,TQ461
  3. Preliminary Study on the Processing Methods of Radix Aconiti,R283
  4. Synthesis of Coptisine from Alkaloids in Coptids Rhizoma with the Similar Structure of Isoquinoline,R284
  5. Domino Reaction of Arylaldehydes and 1-acetylcyclopropane Carboxamides,O621.25
  6. Study on Extraction and Antioxidant Activity of Antioxidant Active Substances from Oat,TS201
  7. Isolation and Analysis of Chemical Components in Catharanthus Roseus (L.) Don,R284
  8. Research of Quality Control About Qingfei Yihuo Wan and Zhizi Jinhua Wan by Capillary Electrophoresis,R286
  9. Study on the Preparation and the Quality Standards of the Wuhuo Depressurization Dripping Pills,TQ461
  10. Studies on Synthesis and Properties of Triazolpyrimidine Derivatives,TQ457.2
  11. High pressure steaming aconite in ester alkaloids in variation research,TQ464.4
  12. Design, Synthesis, and Optoelectronic Properties of Novel Poly-(para-phenylene Vinylene) Derivates (PPVs),O632
  13. Synthesis of Novel Indolizidine Derivatives with an Amino Group,TQ463.53
  14. Pinellia micropropagation and callus elicitors its accumulation of total alkaloids,S567.239
  15. Theoretical Study on the Substitutions of Platinum Complexes with Nonplanar Heterocyclic Piperidine Ligands Binding to Biological Targets,R96
  16. 1 antipsychotic aripiprazole synthesis of 2 isoquinoline derivatives research,R914
  17. Phenolic Alkaloids of Menispermum Dauricum Transdermal Drug Delivery in Vitro,R285
  18. Extraction and Separation of Alkaloids in Aconitum Herbs and Studies of ESI-MS~n on Aconitine-type Alkalaids,R284
  19. The Synthesis of Gem-Difluoromethylenated Analogues of Natural Products,O621.3
  20. Studies on Photosynthetic Characteristics, Cytology and Content of Total Alkaloids of the Genus Lycoris from Anhui Province,S682.29
  21. The Research of the Protection of Yanhusuo Total Alkaloids on Acut Myocardial Ischemia Rats Model of Iso Induction,R285.5

CLC: > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry
© 2012 www.DissertationTopic.Net  Mobile