ANIMAL MODEL;
ARTICLE;
BIOAVAILABILITY;
CONTROLLED STUDY;
DRUG BLOOD LEVEL;
DRUG STABILITY;
DRUG SYNTHESIS;
IN VIVO STUDY;
MALARIA;
MOUSE;
NONHUMAN;
PLASMODIUM BERGHEI;
REACTION ANALYSIS;
SUBSTITUTION REACTION;
ADMINISTRATION, ORAL;
ANIMALS;
ANTIMALARIALS;
ARTEMISININS;
BIOLOGICAL AVAILABILITY;
DRUG RESISTANCE;
DRUG STABILITY;
HETEROCYCLIC COMPOUNDS WITH 4 OR MORE RINGS;
HYDROLYSIS;
MALARIA;
MICE;
PLASMODIUM BERGHEI;
PLASMODIUM FALCIPARUM;
RATS;
RATS, SPRAGUE-DAWLEY;
STEREOISOMERISM;
STRUCTURE-ACTIVITY RELATIONSHIP;
The Chemistry, Pharmacology, and Clinical Applications of Qinghaosu (Artemisinin) and Its Derivatives
Wu, Y. L.; Li, Y. The Chemistry, Pharmacology, and Clinical Applications of Qinghaosu (Artemisinin) and Its Derivatives. Med. Chem. Res. 1995, 5, 599-586.
Studies on Analogs of Artemisinin I. Synthesis of Ethers, Carboxylate Esters and Carbonates of Dihydroartemisinin
Li, Y.; Yu, P. L.; Chen, Y. X.; Li, L. Q.; Gai, Y. Z.; Wang, D. S.; Zheng, Y. P. Studies on Analogs of Artemisinin I. Synthesis of Ethers, Carboxylate Esters and Carbonates of Dihydroartemisinin. Acta Pharm. Sin. 1981, 16, 429-439.
Arteether, a New Antimalarial Drug: Synthesis and Antimalarial Properties
Brossi, A.; Venugopalan, B.; Dominguez Gerpe, L.; Yeh, H. J. C.; Flippen-Anderson, J. L.; Buchs, P.; Luo, X. D.; Milhous, W.; Peters, W. Arteether, a New Antimalarial Drug: synthesis and Antimalarial Properties. J. Med. Chem. 1988, 31, 645-650.
The Chemistry and Synthesis of Qinghaosu Derivatives
China Cooperative Research Group on Qinghaosu and Its Derivatives as Antimalarials. The Chemistry and Synthesis of Qinghaosu Derivatives. J. Trad. Chin. Med. 1982, 2, 9-16.
Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives
Lin, A. J. L.; Klayman, D. L.; Milhous, W. K. Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives. J. Med. Chem. 1987, 30, 2147-2150.
Artemisinin and the Antimalarial Endoperoxides: From Herbal Remedy to Targeted Chemotherapy
Meshnick, S. R.; Taylor, T. E.; Kamchonwongpaisan, S. Artemisinin and the Antimalarial Endoperoxides: From Herbal Remedy to Targeted Chemotherapy. Microbiol. Rev. 1996, 60, 301-315.
Hepatic metabolism of artemisinin drugs: I. Drug metabolism in rat liver microsomes
Leskovac, V.; Theoharides, A. D. Hepatic metabolism of artemisinin drugs: I. Drug metabolism in rat liver microsomes. Comp. Biochem. Physiol. C 1991, 99, 383-390.
Hepatic metabolism of artemisinin drugs: II. Metabolism of arteether in rat liver cytosol
Leskovac, V.; Theoharides, A. D. Hepatic metabolism of artemisinin drugs: II. Metabolism of arteether in rat liver cytosol. Comp. Biochem. Physiol. C 1991, 99, 391-396.
Decomposition of Arteether in Simulated Stomach Acid Yielding Compounds Retaining Antimalarial Activity
Baker, J. K.; McChesney, J. D.; Chi, H. T. Decomposition of Arteether in Simulated Stomach Acid Yielding Compounds Retaining Antimalarial Activity. Pharm. Res. 1993, 10, 662-666.
Current Progress in the Chemistry, Medicinal Chemistry and Drug Design of Artemisinin Based Antimalarials
Vroman, J. A.; Alvim-Gaston, M.; Avery, M. A. Current Progress in the Chemistry, Medicinal Chemistry and Drug Design of Artemisinin Based Antimalarials. Curr. Pharm. Des. 1999, 5, 101-138.
Penetration of Dihydroartemisinin into Cerebrospinal Fluid after Administration of Intravenous Artesunate in Severe Falciparum Malaria
Davis, T. M. E.; Binh, T. Q.; Ilett, K. F.; Batty, K. T.; Phuong, H. L.; Chiswell, G. M.; Phuong, V. D.; Agus, C. Penetration of Dihydroartemisinin into Cerebrospinal Fluid after Administration of Intravenous Artesunate in Severe Falciparum Malaria. Antimicrob. Agents Chemother. 2003, 47, 368-370.
Thirteenth Programme Report of UNDP/World Bank/WHO Special Programme for Research & Training in Tropical Disease (TDR); World Health Organization: Geneva
Tropical Disease Research Progress 1995-96; Thirteenth Programme Report of UNDP/World Bank/WHO Special Programme for Research & Training in Tropical Disease (TDR); World Health Organization: Geneva, 1997; p 97.
Synthesis and Antimalarial Activity of (+)-Deoxoartemisinin
Jung, M.; Li, X.; Bustos, D. A.; ElSohly, H. N.; McChesney, J. D. A.; Milhous, W. K. Synthesis and Antimalarial Activity of (+)-Deoxoartemisinin. J. Med. Chem. 1990, 33, 1516-1518.
Synthesis, Stability, and Antimalarial Activity of New Hydrolytically Stable and Water-Soluble (+)-Deoxoartelinic Acid
Jung, M.; Lee, K.; Kendrick, H.; Robinson, B. L.; Croft, S. L. Synthesis, Stability, and Antimalarial Activity of New Hydrolytically Stable and Water-Soluble (+)-Deoxoartelinic Acid. J. Med. Chem. 2002, 45, 4940-4944.
Synthesis and Antimalarial Activities of 10-Substituted Deoxoartemisinins
Ma, J.; Katz, E.; Kyle, D. E.; Ziffer, H. Synthesis and Antimalarial Activities of 10-Substituted Deoxoartemisinins. J. Med. Chem. 2000, 43, 4228-4232.
Correlation of Antimalarial Activity of Artemisinin Derivatives with Ferroprotoporphyrin IX.J
Pitayatat, S.; Tarnchompoo, B.; Thebtaranonth, Y.; Yuthavong, Y. Correlation of Antimalarial Activity of Artemisinin Derivatives with Ferroprotoporphyrin IX. J. Med. Chem. 1997, 40, 633-638.
C-16-Artemisinin Derivatives and Their Antimalarial and Cytotoxic Activities: Syntheses of Artemisinin Monomers, Dimers, Trimers, and Tetramers by Nucleophilic Additions to Artemisitene
Ekthawatchai, S.; Kamchonwongpaisan, S.; Kongsaeree, P.; Tarnchompoo, B. ; Thebtaranonth, Y.; Yuthavong, Y. C-16-Artemisinin Derivatives and Their Antimalarial and Cytotoxic Activities: Syntheses of Artemisinin Monomers, Dimers, Trimers, and Tetramers by Nucleophilic Additions to Artemisitene. J. Med. Chem. 2001, 44, 4688-4695.
Structure-Activity Relationships of the Antimalarial Agent Artemisinin. 7. Direct Modification of (+)-Artemisinin and in Vivo Antimalarial Sreening of New, Potential Preclinical Antimalarial Candidates
Avery, M. A.; Alvim-Gaston, M.; Vroman, J. A.; Wu, B.; Ager, A.; Peters, W.; Robinson, B. L.; Charman, W. Structure-Activity Relationships of the Antimalarial Agent Artemisinin. 7. Direct Modification of (+)-Artemisinin and in Vivo Antimalarial Sreening of New, Potential Preclinical Antimalarial Candidates. J. Med. Chem. 2002, 45, 4321-4335.
Inhibition of Rat Liver Microsomal Lipid Peroxidation Elicited by 2,2-Dimethylchromenes and Chromans Containing Fluorinated Moieties Resistant to Cytochrome P-450 metabolism
Irurre, J., Jr.; Casas, J.; Ramos, I.; Messeguer, A. Inhibition of Rat Liver Microsomal Lipid Peroxidation Elicited by 2,2-Dimethylchromenes and Chromans Containing Fluorinated Moieties Resistant to Cytochrome P-450 metabolism. Bioorg. Med. Chem. 1993, 1, 219-225.
Resistance of the 2,2,2-trifluoroethoxy aryl moiety to the cytochrome P-450 metabolism in rat liver microsomes
Irurre, J., Jr.; Casas, J.; Messeguer, A. Resistance of the 2,2,2-trifluoroethoxy aryl moiety to the cytochrome P-450 metabolism in rat liver microsomes. Bioorg. Med. Chem. Lett. 1993, 3, 179-182.
Banks, R. E., Smart, B. E., Tatlow, J. C., Eds.; Plenum Press: New York
Edwards, P. N. Uses of Fluorine in Chemotherapy. In Organofluorine Chemistry: Principles and Commercial Applications; Banks, R. E., Smart, B. E., Tatlow, J. C., Eds.; Plenum Press: New York, 1994; pp 501-541.
Synthesis and in Vivo Antimalarial Activity of 12α -Trifluoromethyl-hydroartemisinin
Abouabdellah, A.; Bégué, J. P.; Bonnet-Delpon, D.; Gantier, J. C.; Thanh Nga, T. T.; Truong Dinh, T. Synthesis and in Vivo Antimalarial Activity of 12α-Trifluoromethyl-hydroartemisinin. Bioorg. Biomed. Chem. Lett. 1996, 2717-2720.
Synthesis and Antimalarial Activities of Fluoroalkyl Derivatives of Dihydroartemisinin
Thanh Nga, T. T.; Ménage, C.; Bégué, J. P.; Bonnet-Delpon, D.; Gantier, J. C.; Pradines, B.; Doury, J. C.; Thac, T. D. Synthesis and Antimalarial Activities of Fluoroalkyl Derivatives of Dihydroartemisinin. J. Med. Chem. 1979, 21, 4101-4108.
The Effect of 10α-Trifluoromethyl Hydroartemisinin on Plasmodium berghei Infection and Its Toxicity in Experimental Animals
Binh, P. D.; Cong Le, D.; Nhu, T. V.; Tien, N. T.; Nhan, D. H.; Bégué, J. P.; Bonnet-Delpon, D.; Thanh Nga, T. T. The Effect of 10α-Trifluoromethyl Hydroartemisinin on Plasmodium berghei Infection and Its Toxicity in Experimental Animals. Trans. R. Soc. Trop. Med. Hyg. 2002, 96, 677-683.
Allylic Bromination of Anhydrodihydroartemisinin and of Its 10-Trifluoromethyl Analogue: A New Access to 16-Substituted Artemisinin Derivatives
Grellepois, F.; Chorki, F.; Ourévitch, M.; Crousse, B.; Bonnet-Delpon, D.; Bégué, J. P. Allylic Bromination of Anhydrodihydroartemisinin and of Its 10-Trifluoromethyl Analogue: A New Access to 16-Substituted Artemisinin Derivatives. Tetrahedron Lett. 2002, 43, 7837-7840.
Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives. 2. Stereospecificity of the Ether Side Chain
Lin, A. J.; Lee, M.; Klayman, D. L. Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives. 2. Stereospecificity of the Ether Side Chain. J. Med. Chem. 1989, 32, 1249-1252.
Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives. 3. Aromatic Amine Analogues
Lin, A. J.; Li, L.; Klayman, D. L.; George, C. F.; Flippen-Anderson, J. L. Antimalarial Activity of New Water-Soluble Dihydroartemisinin Derivatives. 3. Aromatic Amine Analogues. J. Med. Chem. 1990, 33, 2610-2614.
Comparison of the Formation Energy of Fluorinated Alkoxycarbenium Ion
Bégué, J. P.; Benayoud, F.; Bonnet-Delpon, D.; Tidwell, T. T.; Cox, R. A.; Allen, A. Comparison of the Formation Energy of Fluorinated Alkoxycarbenium Ion. Gazz. Chim. Ital. 1995, 125, 399-404.
Fluorinated Synthons: Reactivity of 1-Rf-Epoxy Ethers with Lewis Acid
Bégué, J. P.; Benayoud, F.; Bonnet-Delpon, D. Fluorinated Synthons: Reactivity of 1-Rf-Epoxy Ethers with Lewis Acid. J. Org. Chem. 1995, 60, 5029-5036.
Preparation of novel artemisinin derivatives and their use for treating malaria. CNRS Patent PCT/FR02/03675, 25-10-2002
Bégué, J. P.; Bonnet-Delpon, D.; Crousse, B.; Ourévitch, M.; Chorki, F.; Grellepois, F.; Magueur, G. Preparation of novel artemisinin derivatives and their use for treating malaria. CNRS Patent PCT/FR02/03675, 25-10-2002.
Anhydrodihydroartemisinin and Its 10-Trifluoromethyl Analogue: Access to Novel D-Ring Contracted Artemisinin Trifluoromethyl Ketones
Grellepois, F.; Chorki, F.; Crousse, B.; Ourévitch, M.; Bonnet-Delpon, D.; Bégué, J. P. Anhydrodihydroartemisinin and Its 10-Trifluoromethyl Analogue: Access to Novel D-Ring Contracted Artemisinin Trifluoromethyl Ketones. J. Org. Chem. 2002, 67, 1253-1260.
Quantitive Assessment of Antimalarial Activity in Vitro by a Semiautomated Microdilution Technique Antimicrob
Desjardins, R. E.; Canfield, C. J.; Haynes, J. D.; Chulay, D. J. Quantitive Assessment of Antimalarial Activity in Vitro by a Semiautomated Microdilution Technique Antimicrob. Agents Chemother. 1979, 16, 710-718.
Techniques of drug evaluation I: Primary screening
Peters, W., Ed.; Academic Press: London
Peters, W. Techniques of drug evaluation I: primary screening. In Chemotherapy and Drug Resistance in Malaria; Peters, W., Ed.; Academic Press: London, 1987; Vol. 1, pp 100-123.