Dissertation > Excellent graduate degree dissertation topics show

Synthesis and Anti-malarial Activity in Vivo of Naphthoquine Derivatives

Author: TangLing
Tutor: WangHongQuan
School: Central South University
Course: Pharmacy
Keywords: Naphthoquine derivatives 4-aminoquinoline antimalarialactivity in vitro Plasmodium berghei Keyberg173strain Mannich naphthaoxazine
CLC: TQ460.1
Type: Master's thesis
Year: 2013
Downloads: 3
Quote: 0
Read: Download Dissertation

Abstract


Naphthoquine (NQ) is a4’-hydroxyphenyl amino quinoline antimalarial developed in our lab. It is indicated that NQ has a high efficacy and good compliance of patients owe to its long half-life. Combined with artemisinin, it is a new fixed-dose ACT named ARCO(?) which is the only single-dose ACT available at present. Long half-life also make resistance formed easier. Experimental results show that the resistant mechanism of NQ is same with CQ. To afford multiple selections is necessary by searching for novel derivates base on NQ.We chose three kinds of terminal side chains to carry out modification terminal side chain with mannich base derivatives on phenol hydroxyl ortho-position of NQ:long chain alkoxy amines, long chain hydroxy-alkyl-amine, nitric heterocyclic ring compounds.We synthesized25new derivatives and determined their meting points (mp). The1H NMR and Mass Spectra were obtained to certify structure. All compounds were tested in vitro against parasite strains K173using’4-day inhibiton assays’and calculate the ED50.The ED50of Compound11is similar with NQ while compound20is less than NQ. The change on structure shows little relevant with anti-malarial activity.

Related Dissertations

  1. Aza polydentate metal Complexes,O627
  2. Theoretical study of small organic molecules catalyzed asymmetric reactions,O621.251
  3. Study on Mannich Reaction Induced by Radical Cation Salts and Catalyzed by InCl3.4H2O,O643.32
  4. Study on the Thiourea and Benzotriazole Mannich Alkali Corrosion Inhibition for Copper in Alkali Medium,TG174.42
  5. The Synthesis and Application of a Phenol-Based Mannich Polyol,TQ243.4
  6. Synthesis, Structure and Magnetic Properties of Amine Bis(Phenolate) Copper (Ⅱ) Complex,O627.12
  7. Three-component One-pot Mannich Reactions Catalyzed by Novel Envirorment-friendly Catalysts,O643.32
  8. Synthesis and activity of curcumin Mannich base derivatives,R284
  9. The Asymmetric Autocatalysis of Mannich Reaction,O643.32
  10. Synthesis and Evaluation of the Thinner for Drilling Fluid,TE254
  11. Study on Synthesis of the Novel 2,3-pyridine-dione,O626
  12. Tandem Mannich reaction and oxime compounds of O- alkylation,O621.25
  13. Chiral Br (?) Nsted acid catalyst Catalytic Asymmetric Synthesis and Reactions,O621.25
  14. Study on Synthesis of N-Alkyl-Substituted-4-Piperidones,TQ252
  15. Synthesis and in Vitro Antioxidant Capacities Assay of Xanthonic Derivatives,R96
  16. Synthesis and Antitumor Acitivity of Novel Isoliquiritigenin Analogues,TQ463
  17. Electrolytic preparation and application of ionic liquids,X703
  18. Studies on Synthesis and Biological Activity of 2-substituted of Cephalosporin New Compounds,R96
  19. The Synthesis of Ethyl 5-methyl-3-quinoxalinyl-isoxazole-4-carboxylate and Their Derivatives,O626
  20. Studies on Synthesis of Polysubstituted Tetrahydropyridens Via Multicomponent Reactions of Brassard’s Diene, Aldehydes and Anilines,O626.32
  21. Studies on the Synthesis of 3-Alkylindoles,O626

CLC: > Industrial Technology > Chemical Industry > Pharmaceutical chemical industry > General issues > Basic theory
© 2012 www.DissertationTopic.Net  Mobile