In vitro activities of DU-1102, a new trioxaquine derivative, against Plasmodium falciparum isolates

Antimicrobial Agents and Chemotherapy

Volumn 45, Issue 6, 2001, Pages 1886-1888

  Basco, Leonardo K ^a   Dechy Cabaret, Odile ^b   Ndounga, Mathieu ^a   Meche, Fleurette Solange ^a   Robert, Anne ^b   Meunier, Bernard ^b  

^a Laboratoire de Recherche sur le Paludisme Yaounde   (Cameroon)

^b LCC LABORATOIRE DE CHIMIE DE COORDINATION   (France)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOQUINOLINE DERIVATIVE; ARTEMISININ DERIVATIVE; CHLOROQUINE; DU 1102; PYRIMETHAMINE; QUININE DERIVATIVE; TRIOXAQUINE DERIVATIVE; UNCLASSIFIED DRUG;

ANTIMALARIAL ACTIVITY; ARTICLE; COVALENT BOND; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; IN VITRO STUDY; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; STRUCTURE ANALYSIS;

AMINOQUINOLINES; ANIMALS; ANTIMALARIALS; BICYCLO COMPOUNDS, HETEROCYCLIC; CHLOROQUINE; PLASMODIUM FALCIPARUM; PYRIMETHAMINE; REGRESSION ANALYSIS;

EID: 0035020671     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.45.6.1886-1888.2001     Document Type: Article

References (19)

1. Avery, M. A., F. Gao, W. K. M. Chong, S. Mehrotra, and W. K. Milhous. 1993. Structure-activity relationships of the antimalarial artemisinin. I. Synthesis and comparative molecular field analysis of C-9 analogs of artemisinin and 10-deoxoartemisinin. J. Med. Chem. 36:4264-4275.
2. Basco, L. K., J. Bickii, and P. Ringwald. 1998. In vitro activity of lumefantrine (benflumetol) against clinical isolates of Plasmodium falciparum in Yaoundé, Cameroon. Antimicrob. Agents Chemother. 42:2347-2351.
3. Basco, L. K., and P. Ringwald. 1999. Molecular epidemiology of malaria in Yaounde, Cameroon. IV. Evolution of pyrimethamine resistance between 1994 and 1998. Am. J. Trop. Med. Hyg. 61:802-806.
4. Cazelles, J., A. Robert, and B. Meunier. 2001. Alkylation of heme by artemisinin, an antimalarial drug. C. R. Acad. Sci. Ser. II C 4:85-89.
5. Cumming, J. N., P. Ploypradith, and G. H. Posner. 1997. Antimalarial activity of artemisinin (quinghaosu) and related trioxanes: mechanism(s) of action. Adv. Pharmacol. 37:253-297.
6. Cumming, J. N., D. Wang, S. B. Park, T. A. Shapiro, and G. H. Posner. 1998. Design, synthesis, derivatization, and structure-activity relationships of simplified, tricyclic, 1,2,4-trioxane-alcohol analogues of the antimalarial artemisinin. J. Med. Chem. 41:952-964.
7. Dechy-Cabaret, O., F. Benoit-Vical, A. Robert, and B. Meunier. 2000. Preparation and antimalarial activities of "trioxaquines", new modular molecules with a trioxane skeleton linked to a 4-aminoquinoline. ChemBio Chem 1:281-283.
8. Desjardins, R. E., C. J. Canfield, J. D. Haynes, and J. D. Chulay. 1979. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob. Agents Chemother. 16:710-718.
9. Egan, T. J., and H. M. Marques. 1999. The role of haem in the activity of chloroquine and related antimalarial drugs. Coord. Chem. Rev. 190-192: 493-517.
10. Meshnick, S. R., T. E. Taylor, and S. Kamchonwongpaisan. 1996. Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy. Microbiol. Rev. 60:301-315.
11. Meunier, B., A. Robert, O. Dechy-Cabaret, and F. Benoit-Vical. April 2000. French patent 0004422.
12. Mount, D. L., B. L. Nahlen, L. C. Patchen, and F. C. Churchill. 1989. Adaptations of the Saker-Solomons test: simple, reliable colorimetric field assays for chloroquine and its metabolites in urine. Bull. W.H.O. 67:295-300.
13. Peters, W. 1990. The prevention of antimalarial drug resistance. Pharmacol. Ther. 47:499-508.
14. Ringwald, P., J. Bickii, and L. Basco. 1996. Randomised trial of pyronaridine versus chloroquine for acute uncomplicated falciparum malaria in Africa. Lancet 347:24-28.
15. Robert, A., and B. Meunier. 1997. Characterization of the first covalent adduct between artemisinin and a henie model. J. Am. Chem. Soc. 119:5968-5969.
16. Robert, A., and B. Meunier. 1998. Alkylating properties of antimalarial artemisinin derivatives and synthetic trioxanes when activated by a reduced heme model. Chem. Eur. J. 4:1287-1296.
17. Robert, A., and B. Meunier. 1998. Is alkylation the main mechanism of action of the antimalarial drug artemisinin? Chem. Soc. Rev. 27:273-279.
18. Vroman, J. A., M. Alvim-Gaston, and M. A. Avery. 1999. Current progress in the chemistry, medicinal chemistry and drug design of artemisinin based antimalarials. Curr. Pharm. Des. 5:101-138.
19. White, N. J., and P. L. Olliaro. 1996. Strategies for the prevention of antimalarial drug resistance: rationale for combination chemotherapy for malaria. Parasitol. Today 12:399-401.